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1.
Molecules ; 28(2)2023 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-36677613

RESUMEN

These days an extensive amount of the attention of researchers is focused towards exploring bioactive compounds of natural or herbal origin for therapeutic intervention in different ailments of significant importance. One such novel bioactive compound that has a variety of biological properties, including anti-inflammatory and antioxidant activities, is piperine. However, until today, piperine has not been explored for its potential to improve inflammation and enhance healing in acute and chronic wounds. Therefore, the present study aimed to investigate the wound healing potential of piperine hydrogel formulation after topical application. Hydrogels fit the need for a depot system at the wound bed, where they ensure a consistent supply of therapeutic agents enclosed in their cross-linked network matrices. In the present study, piperine-containing carbopol 934 hydrogels mixed with Aloe vera gels of different gel strengths were prepared and characterized for rheological behavior, spreadability, extrudability, and percent (%) content uniformity. Furthermore, the wound healing potential of the developed formulation system was explored utilizing the excision wound healing model. The results of an in vivo study and histopathological examination revealed early and intrinsic healing of wounds with the piperine-containing bioactive hydrogel system compared to the bioactive hydrogel system without piperine. Therefore, the study's findings establish that the piperine-containing bioactive hydrogel system is a promising therapeutic approach for wound healing application that should be diligently considered for clinical transferability.


Asunto(s)
Alcaloides , Hidrogeles , Ratas , Animales , Hidrogeles/farmacología , Piel/patología , Cicatrización de Heridas , Alcaloides/farmacología , Alcaloides/uso terapéutico
2.
Molecules ; 28(3)2023 Jan 26.
Artículo en Inglés | MEDLINE | ID: mdl-36770883

RESUMEN

Immunotherapy shows a lot of promise for addressing the problems with traditional cancer treatments. Researchers and clinicians are working to create innovative immunological techniques for cancer detection and treatment that are more selective and have lower toxicity. An emerging field in cancer therapy, immunomodulation offers patients an alternate approach to treating cancer. These therapies use the host's natural defensive systems to identify and remove malignant cells in a targeted manner. Cancer treatment is now undergoing somewhat of a revolution due to recent developments in nanotechnology. Diverse nanomaterials (NMs) have been employed to overcome the limits of conventional anti-cancer treatments such as cytotoxic, surgery, radiation, and chemotherapy. Aside from that, NMs could interact with live cells and influence immune responses. In contrast, unexpected adverse effects such as necrosis, hypersensitivity, and inflammation might result from the immune system (IS)'s interaction with NMs. Therefore, to ensure the efficacy of immunomodulatory nanomaterials, it is essential to have a comprehensive understanding of the intricate interplay that exists between the IS and NMs. This review intends to present an overview of the current achievements, challenges, and improvements in using immunomodulatory nanomaterials (iNMs) for cancer therapy, with an emphasis on elucidating the mechanisms involved in the interaction between NMs and the immune system of the host.


Asunto(s)
Antineoplásicos , Nanoestructuras , Neoplasias , Humanos , Nanoestructuras/uso terapéutico , Nanotecnología , Antineoplásicos/uso terapéutico , Inmunoterapia , Neoplasias/tratamiento farmacológico
3.
Molecules ; 27(22)2022 Nov 09.
Artículo en Inglés | MEDLINE | ID: mdl-36431808

RESUMEN

Diabetes mellitus is one of the most prevalent metabolic disorders characterized by hyperglycemia due to impaired glucose metabolism. Overproduction of free radicals due to chronic hyperglycemia may cause oxidative stress, which delays wound healing in diabetic conditions. For people with diabetes, this impeded wound healing is one of the predominant reasons for mortality and morbidity. The study aimed to develop an Ocimum sanctum leaf extract-mediated green synthesis of titanium dioxide (TiO2) nanoparticles (NPs) and further incorporate them into 2% chitosan (CS) gel for diabetic wound healing. UV-visible spectrum analysis recorded the sharp peak at 235 and 320 nm, and this was the preliminary sign for the biosynthesis of TiO2 NPs. The FTIR analysis was used to perform a qualitative validation of the biosynthesized TiO2 nanoparticles. XRD analysis indicated the crystallinity of TiO2 NPs in anatase form. Microscopic investigation revealed that TiO2 NPs were spherical and polygonal in shape, with sizes ranging from 75 to 123 nm. The EDX analysis of green synthesized NPs showed the presence of TiO2 NPs, demonstrating the peak of titanium ion and oxygen. The hydrodynamic diameter and polydispersity index (PDI) of the TiO2 NPs were found to be 130.3 nm and 0.237, respectively. The developed TiO2 NPs containing CS gel exhibited the desired thixotropic properties with pseudoplastic behavior. In vivo wound healing studies and histopathological investigations of healed wounds demonstrated the excellent wound-healing efficacy of TiO2 NPs containing CS gel in diabetic rats.


Asunto(s)
Diabetes Mellitus Experimental , Hiperglucemia , Nanopartículas , Aceites Volátiles , Ratas , Animales , Titanio/farmacología , Ocimum sanctum/metabolismo , Diabetes Mellitus Experimental/tratamiento farmacológico , Nanopartículas/ultraestructura , Cicatrización de Heridas , Extractos Vegetales/farmacología , Extractos Vegetales/metabolismo
4.
Molecules ; 27(4)2022 Feb 18.
Artículo en Inglés | MEDLINE | ID: mdl-35209180

RESUMEN

Bionanotechnology is a branch of science that has revolutionized modern science and technology. Nanomaterials, especially noble metals, have attracted researchers due to their size and application in different branches of sciences that benefit humanity. Metal nanoparticles can be synthesized using green methods, which are good for the environment, economically viable, and facilitate synthesis. Due to their size and form, gold nanoparticles have become significant. Plant materials are of particular interest in the synthesis and manufacture of theranostic gold nanoparticles (NPs), which have been generated using various materials. On the other hand, chemically produced nanoparticles have several drawbacks in terms of cost, toxicity, and effectiveness. A plant-mediated integration of metallic nanoparticles has been developed in the field of nanotechnology to overcome the drawbacks of traditional synthesis, such as physical and synthetic strategies. Nanomaterials' tunable features make them sophisticated tools in the biomedical platform, especially for developing new diagnostics and therapeutics for malignancy, neurodegenerative, and other chronic disorders. Therefore, this review outlines the theranostic approach, the different plant materials utilized in theranostic applications, and future directions based on current breakthroughs in these fields.


Asunto(s)
Oro , Tecnología Química Verde , Nanopartículas del Metal , Extractos Vegetales , Nanomedicina Teranóstica/métodos , Fenómenos Químicos , Técnicas de Química Sintética , Desarrollo de Medicamentos , Oro/química , Tecnología Química Verde/métodos , Humanos , Nanopartículas del Metal/química , Nanopartículas del Metal/ultraestructura , Nanotecnología , Extractos Vegetales/química , Plantas Medicinales/química , Análisis Espectral
5.
Molecules ; 26(13)2021 Jun 24.
Artículo en Inglés | MEDLINE | ID: mdl-34202733

RESUMEN

Thymoquinone is a natural bioactive with significant therapeutic activity against multiple ailments including wound healing. The poor aqueous solubility and low skin permeability limit its therapeutic efficacy. The present investigation aimed to improve the biopharmaceutical attributes of thymoquinone to enhance its topical efficacy in wound healing. A nanoemulsion-based hydrogel system was designed and characterized as a nanotechnology-mediated drug delivery approach to improve the therapeutic efficacy of thymoquinone, utilizing a high-energy emulsification technique. The black seed oil, as a natural home of thymoquinone, was utilized to improve the drug loading capacity of the developed nanoemulsion system and reduced the oil droplet size to <100 nm through ultrasonication. The influence of formulation composition, and the ultrasonication process conditions, were investigated on the mean globule size and polydispersity index of the generated nanoemulsion. Irrespective of surfactant/co-surfactant ratio and % concentration of surfactant/co-surfactant mixture, the ultrasonication time had a significant (p < 0.05) influence on the mean droplet size and polydispersity index of the generated nanoemulsion. The developed nanoemulgel system of thymoquinone demonstrated the pseudoplastic behavior with thixotropic properties, and this behavior is desirable for topical application. The nanoemulgel system of thymoquinone exhibited significant enhancement (p < 0.05) in skin penetrability and deposition characteristics after topical administration compared to the conventional hydrogel system. The developed nanoemulgel system of thymoquinone exhibited quicker and early healing in wounded Wistar rats compared to the conventional hydrogel of thymoquinone, while showing comparable healing efficacy with respect to marketed silver sulfadiazine (1%) cream. Furthermore, histopathology analysis of animals treated with a developed formulation system demonstrated the formation of the thick epidermal layer, papillary dermis along with the presence of extensive and organized collagen fibers in newly healed tissues. The outcome of this investigation signifies that topical delivery of thymoquinone through nanoemulgel system is a promising candidate which accelerates the process of wound healing in preclinical study.


Asunto(s)
Benzoquinonas , Sistemas de Liberación de Medicamentos , Nanopartículas , Absorción Cutánea/efectos de los fármacos , Piel/metabolismo , Cicatrización de Heridas/efectos de los fármacos , Administración Tópica , Animales , Benzoquinonas/química , Benzoquinonas/farmacocinética , Benzoquinonas/farmacología , Emulsiones , Nanopartículas/química , Nanopartículas/uso terapéutico , Ratas , Ratas Wistar , Piel/patología
6.
Pharm Dev Technol ; 22(3): 302-311, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-26794727

RESUMEN

Rapid advancement in the field of colloidal science has shown a great progress in the development of proniosome technology (PT) as an impending drug delivery system. PT is a valuable carrier system for delivery of hydrophobic as well as hydrophilic drugs. It is a liquid crystalline compact niosomal hybrid, which upon hydration gives niosomes. They can augment the bioavailability of encapsulated drug and provide better therapeutic activity in a controlled manner. Non-toxicity, penetration enhancing the effect of surfactant and modified drug release from the proniosomal transdermal gel has attracted a greater attention of formulation scientist toward PT. Free flowing dry proniosomal powder are suitable for unit dosage forms such as tablet and capsules. Proniosomes are auspicious drug delivery system for the future. Proniosomes-derived niosomes are a better alternative to the other vesicular system due to their superior physicochemical stability and effective drug delivery capability. The focus of this review is to bring out all the aspects of proniosomes including their different compositions, various methods of preparation, characterization and recent development in their therapeutic applications.


Asunto(s)
Composición de Medicamentos/métodos , Geles/química , Liposomas/química , Preparaciones Farmacéuticas/administración & dosificación , Administración Cutánea , Administración por Inhalación , Administración Oral , Animales , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/química , Liberación de Fármacos , Liposomas/administración & dosificación , Propiedades de Superficie
7.
Pharm Dev Technol ; 19(4): 460-7, 2014 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-23675949

RESUMEN

Collagen, a high molecular weight, hydrophilic and highly abundant protein is known to have anti-ageing, anti-wrinkle, anti-acne, anti-scar and wound healing properties. High molecular weight and hydrophilic nature hinder its effective topical delivery. So, the objective of present study was to develop effective topical nano-surfactant dispersion (NSD) for collagen delivery. NSD was prepared from sorbitan monostearate (Span60) and cholesterol using ethanol injection method followed by probe sonication. NSD was characterized for entrapment efficiency (%EE), size and size distribution (Z-avg and polydispersity index (PDI)), shape, zeta-potential (ζ), in vitro drug release, skin hydration and skin irritation test and histopathological examination. Optimized NSD (NSD3) had %EE, z-avg, PDI and ζ-potential of 77.56% ± 1.09%, 158.1 ± 2.31 nm, 0.211 and -17.2 ± 0.64 mV, respectively. In in vivo skin hydration test, NSD treatment showed nearly 2.5-fold and 3-fold increase in the thickness of stratum corneum (SC) as compared to the collagen gel treated and untreated skin, respectively. The mean scores of skin irritation test in two animal species, rats and rabbits, were found to be 1.42 ± 1.01 and 1.71 ± 0.29, respectively, indicating the non-irritant nature of collagen loaded NSD. Histopathology of the skin after application of developed NSD showed non-significant changes in skin anatomy indicating its safe nature.


Asunto(s)
Colágeno/administración & dosificación , Colágeno/química , Nanopartículas/administración & dosificación , Nanopartículas/química , Tensoactivos/administración & dosificación , Tensoactivos/química , Animales , Química Farmacéutica/métodos , Colesterol/administración & dosificación , Colesterol/química , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Geles/administración & dosificación , Geles/química , Hexosas/administración & dosificación , Hexosas/química , Masculino , Tamaño de la Partícula , Conejos , Ratas , Ratas Wistar , Piel/metabolismo , Absorción Cutánea
8.
Expert Opin Drug Deliv ; 21(2): 229-244, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38344809

RESUMEN

INTRODUCTION: Triple-negative breast cancer (TNBC) presents unique challenges in diagnosis and treatment. Resveratrol exhibits potential as a therapeutic intervention against TNBC by regulating various pathways such as the PI3K/AKT, RAS/RAF/ERK, PKCδ, and AMPK, leading to apoptosis through ROS-mediated CHOP activationand the expression of DR4 and DR5. However, the clinical efficacy of resveratrol is limited due to its poor biopharmaceutical characteristics and low bioavailability at the tumor site. Nanotechnology offers a promising approach to improving the biopharmaceutical characteristics of resveratrol to achieve clinical efficacy in different cancers. The small dimension (<200 nm) of nanotechnology-mediated drug delivery system is helpful to improve the bioavailability, internalization into the TNBC cell, ligand-specific targeted delivery of loaded resveratrol to tumor site including reversal of MDR (multi-drug resistance) condition. AREAS COVERED: This manuscript provides a comprehensive discussion on the structure-activity relationship (SAR), underlying anticancer mechanism, evidence of anticancer activity in in-vitro/in-vivo investigations, and the significance of nanotechnology-mediated delivery of resveratrol in TNBC. EXPERT OPINION: Advanced nano-formulations of resveratrol such as oxidized mesoporous carbon nanoparticles, macrophage-derived vesicular system, functionalized gold nanoparticles, etc. have increased the accumulation of loaded therapeutics at the tumor-site, and avoid off-target drug release. In conclusion, nano-resveratrol as a strategy may provide improved tumor-specific image-guided treatment options for TNBC utilizing theranostic approach.


Asunto(s)
Productos Biológicos , Nanopartículas del Metal , Nanopartículas , Neoplasias de la Mama Triple Negativas , Humanos , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/metabolismo , Neoplasias de la Mama Triple Negativas/patología , Resveratrol/uso terapéutico , Oro , Fosfatidilinositol 3-Quinasas/uso terapéutico , Nanotecnología , Línea Celular Tumoral , Nanopartículas/metabolismo
9.
Med Chem ; 20(1): 78-91, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-37594099

RESUMEN

INTRODUCTION: Inflammation can be defined as a complex biological response that is produced by body tissues to harmful agents like pathogens, irritants, and damaged cells and thereby acts as a protective response incorporating immune cells, blood vessels, and molecular mediators. Histamine, serotonin, bradykinin, leukotrienes (LTB4), prostaglandins (PGE2), prostacyclins, reactive oxygen species, proinflammatory cytokines like IL-1, IL-11, TNF- anti-inflammatory cytokines like IL-4, IL-10, IL-11, IL-6 and IL-13, etc. all have different effects on both pro and anti-inflammatory mediators. Incorporation of combinatorial chemistry and computational studies have helped the researchers to design xanthones moieties with high selectivity that can serve as a lead compound and help develop potential compounds that can act as effective COX-2 inhibitors. The study aims to design and develop different series of substituted hydroxyxanthone derivatives with anti-inflammatory potential. METHODS: The partially purified synthetic xanthone derivatives were orally administered to the carrageenan induced paw oedemic rat models at the dose of 100 mg/kg, and their effect in controlling the degree of inflammation was measured at the time interval of 30 min, 1, 2, 3, 4 and 6 hrs. respectively. Further, these compounds were also subjected to modern analytical studies like UV, IR, NMR and mass spectrometry or their characterization. RESULTS: The results drawn out of the in silico, in vitro, in vivo and analytical studies concluded that the hydroxyxanthone derivatives can obstruct the enzyme COX-2 and produce anti-inflammatory action potentially. CONCLUSION: With the aim to evaluate the compounds for their anti-inflammatory activity, it was observed that the newly designed xanthonic compounds also possess a safe toxicity margin and hence can be utilized by the researchers to develop hybrid xanthonic moieties that can specifically target the enzyme COX-2.


Asunto(s)
Inhibidores de la Ciclooxigenasa 2 , Xantonas , Animales , Ratas , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Carragenina/uso terapéutico , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2/farmacología , Citocinas , Edema/inducido químicamente , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Interleucina-11/metabolismo , Relación Estructura-Actividad Cuantitativa , Xantonas/farmacología
10.
Int J Biol Macromol ; 257(Pt 1): 128573, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38052290

RESUMEN

This study explores the eco-friendly biosynthesis of silver nanoparticles (AgNPs) utilizing Camellia sinensis leaf extract. We assess their antioxidant and antibacterial properties. Furthermore, we impregnated AgNPs into 2 % chitosan (CHS) gel and assessed their wound-healing potential in Escherichia coli and Staphylococcus aureus infected wounds. Optimized AgNPs demonstrated a mean particle size of 36.90 ± 1.22 nm and a PDI of 0.049 ± 0.001. Green-synthesized AgNPs exhibited enhanced free radical inhibition (IC50: 31.45 µg/mL, 34.01 µg/mL, 27.40 µg/mL) compared to leaf extract (IC50: 52.67 µg/mL, 59.64 µg/mL, 97.50 µg/mL) in DPPH, hydrogen peroxide, and nitric oxide free radical scavenging assays, respectively. The MIC/MBC values of AgNPs against E. coli and S. aureus were 5 ppm/ 7.5 ppm and 10 ppm/ 15 ppm, respectively. Furthermore, our study showed that green-synthesized AgNPs at MIC significantly reduced the biofilm production of E. coli (70.37 %) and S. aureus (67.40 %). The CHS/AgNPs gel exhibited potent wound healing activities, comparable to a commercial cream with the re-epithelialization period of 8.16 ± 0.75. Histological analysis demonstrated enhanced skin regeneration with a thicker epidermal layer, well-defined papillary dermal structure, and organized collagen fibers. In summary, these findings hold promise for addressing bacterial infections, particularly those associated with biofilms-related wound infections.


Asunto(s)
Camellia sinensis , Quitosano , Nanopartículas del Metal , Plata/química , Staphylococcus aureus , Quitosano/química , Nanopartículas del Metal/química , Escherichia coli , Antibacterianos/química , Radicales Libres , Extractos Vegetales/farmacología , Extractos Vegetales/química , Pruebas de Sensibilidad Microbiana
11.
Artículo en Inglés | MEDLINE | ID: mdl-38551038

RESUMEN

Alzheimer's disease (AD) is a prevalent neurodegenerative disorder affecting elderly individuals, characterized by progressive cognitive decline leading to dementia. This review examines the challenges posed by anatomical and biochemical barriers such as the blood-brain barrier (BBB), blood-cerebrospinal fluid barrier (BCSFB), and p-glycoproteins in delivering effective therapeutic agents to the central nervous system (CNS) for AD treatment. This article outlines the fundamental role of acetylcholinesterase inhibitors (AChEIs) and NMDA(N-Methyl-D-Aspartate) receptor antagonists in conventional AD therapy and highlights their limitations in terms of brain-specific delivery. It delves into the intricacies of BBB and pglycoprotein-mediated efflux mechanisms that impede drug transport to the CNS. The review further discusses cutting-edge nanomedicine-based strategies, detailing their composition and mechanisms that enable effective bypassing of BBB and enhancing drug accumulation in brain tissues. Conventional therapies, namely AChEIs and NMDA receptor antagonists, have shown limited efficacy and are hindered by suboptimal brain penetration. The advent of nanotechnology-driven therapeutic delivery systems offers promising strategies to enhance CNS targeting and bioavailability, thereby addressing the shortcomings of conventional treatments. Various nanomedicines, encompassing polymeric and metallic nanoparticles (MNPs), solid lipid nanoparticles (SLNs), liposomes, micelles, dendrimers, nanoemulsions, and carbon nanotubes, have been investigated for their potential in delivering anti-AD agents like AChEIs, polyphenols, curcumin, and resveratrol. These nanocarriers exhibit the ability to traverse the BBB and deliver therapeutic payloads to the brain, thereby holding immense potential for effective AD treatment and early diagnostic approaches. Notably, nanocarriers loaded with AChEIs have shown promising results in preclinical studies, exhibiting improved therapeutic efficacy and sustained release profiles. This review underscores the urgency of innovative drug delivery approaches to overcome barriers in AD therapy. Nanomedicine-based solutions offer a promising avenue for achieving effective CNS targeting, enabling enhanced bioavailability and sustained therapeutic effects. As ongoing research continues to elucidate the complexities of CNS drug delivery, these advancements hold great potential for revolutionizing AD treatment and diagnosis.

12.
Drug Dev Ind Pharm ; 39(12): 1936-43, 2013 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-23013140

RESUMEN

The purpose of this investigation was to evaluate the colon-targeted Irinotecan Hydrochloride (ITC-HCl) loaded microspheres by pharmacokinetic and biochemical studies. The microspheres were prepared by double emulsion solvent evaporation method with natural polymer Assam Bora rice starch. The microspheres were characterized for their micromeritics properties, incorporation efficiency, in vitro and in vivo drug release studies. The release study confirmed the insignificant release of ITC-HCl in physiological condition of stomach and small intestine and major drug release in the caecal content. In vivo release study of the optimized microsphere was compared with immediate release (IR) ITC-HCl. ITC-HCl was distributed predominantly in the upper GI tract from the IR, whereas ITC-HCl was distributed primarily to the lower part of GI tract from the microspheres formulation. Enhanced levels of liver enzymes were found in animals given IR ITC-HCl as well as augmented levels of serum albumin, creatinine, leucocytopenia and thrombocytopenia was also observed. In summary, Assam Bora rice starch microspheres exhibit slow and extended release of ITC-HCl over longer periods of time with reduced systemic side-effects.


Asunto(s)
Camptotecina/análogos & derivados , Colon/metabolismo , Microesferas , Almidón/química , Animales , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/farmacocinética , Antineoplásicos Fitogénicos/toxicidad , Camptotecina/administración & dosificación , Camptotecina/farmacocinética , Camptotecina/toxicidad , Química Farmacéutica , Neoplasias Colorrectales/tratamiento farmacológico , Emulsiones , Tracto Gastrointestinal/metabolismo , Irinotecán , Hígado/enzimología , Masculino , Oryza/química , Ratas , Solventes/química , Factores de Tiempo , Distribución Tisular
13.
3 Biotech ; 13(3): 101, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36860361

RESUMEN

Exosomes are nanosized (size ~ 30-150 nm) natural vesicular structures released from cells by physiological processes or pathological circumstances. Exosomes are growing in popularity as a result of their many benefits over conventional nanovehicles, including their ability to escape homing in the liver or metabolic destruction and their lack of undesired accumulation before reaching their intended targets. Various therapeutic molecules, including nucleic acids, have been incorporated into exosomes by different techniques, many of which have shown satisfactory performance in various diseases. Surface-modified exosomes are a potentially effective strategy, and it increases the circulation time and produces the specific drug target vehicle. In this comprehensive review, we describe composition exosomes biogenesis and the role of exosomes in intercellular signaling and cell-cell communications, immune responses, cellular homeostasis, autophagy, and infectious diseases. In addition, we discuss the role of exosomes as diagnostic markers, and their therapeutic and clinical implications. Furthermore, we addressed the challenges and outstanding developments in exosome research and discuss future perspectives. In addition to the current status of exosomes as a therapeutic carrier, the lacuna in the clinical development lifecycles along with the possible strategies to fill the lacuna have been addressed.

14.
Pharmaceutics ; 15(5)2023 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-37242690

RESUMEN

3D printing technology in medicine is gaining great attention from researchers since the FDA approved the first 3D-printed tablet (Spritam®) on the market. This technique permits the fabrication of various types of dosage forms with different geometries and designs. Its feasibility in the design of different types of pharmaceutical dosage forms is very promising for making quick prototypes because it is flexible and does not require expensive equipment or molds. However, the development of multi-functional drug delivery systems, specifically as solid dosage forms loaded with nanopharmaceuticals, has received attention in recent years, although it is challenging for formulators to convert them into a successful solid dosage form. The combination of nanotechnology with the 3D printing technique in the field of medicine has provided a platform to overcome the challenges associated with the fabrication of nanomedicine-based solid dosage forms. Therefore, the major focus of the present manuscript is to review the recent research developments that involved the formulation design of nanomedicine-based solid dosage forms utilizing 3D printing technology. Utilization of 3D printing techniques in the field of nanopharmaceuticals achieved the successful transformation of liquid polymeric nanocapsules and liquid self-nanoemulsifying drug delivery systems (SNEDDS) to solid dosage forms such as tablets and suppositories easily with customized doses as per the needs of the individual patient (personalized medicine). Furthermore, the present review also highlights the utility of extrusion-based 3D printing techniques (Pressure-Assisted Microsyringe-PAM; Fused Deposition Modeling-FDM) to produce tablets and suppositories containing polymeric nanocapsule systems and SNEDDS for oral and rectal administration. The manuscript critically analyzes contemporary research related to the impact of various process parameters on the performance of 3D-printed solid dosage forms.

15.
Pharmaceutics ; 15(2)2023 Feb 17.
Artículo en Inglés | MEDLINE | ID: mdl-36840002

RESUMEN

Glaucoma is a degenerative, chronic ocular disease that causes irreversible vision loss. The major symptom of glaucoma is high intraocular pressure, which happens when the flow of aqueous humor between the front and back of the eye is blocked. Glaucoma therapy is challenging because of the low bioavailability of drugs from conventional ocular drug delivery systems such as eye drops, ointments, and gels. The low bioavailability of antiglaucoma agents could be due to the precorneal and corneal barriers as well as the low biopharmaceutical attributes of the drugs. These limitations can be overcome by employing nanoparticulate drug delivery systems. Over the last decade, there has been a lot of interest in chitosan-based nanoparticulate systems to overcome the limitations (such as poor residence time, low corneal permeability, etc.) associated with conventional ocular pharmaceutical products. Therefore, the main aim of the present manuscript is to review the recent research work involving the chitosan-based nanoparticulate system to treat glaucoma. It discusses the significance of the chitosan-based nanoparticulate system, which provides mucoadhesion to improve the residence time of drugs and their ocular bioavailability. Furthermore, different types of chitosan-based nanoparticulate systems are also discussed, namely nanoparticles of chitosan core only, nanoparticles coated with chitosan, and hybrid nanoparticles of chitosan. The manuscript also provides a critical analysis of contemporary research related to the impact of this chitosan-based nanomedicine on the corneal permeability, ocular bioavailability, and therapeutic performance of loaded antiglaucoma agents.

16.
J Cosmet Dermatol ; 22(4): 1220-1232, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36606411

RESUMEN

BACKGROUND: Scar formation is undesirable both cosmetically and functionally. It shows that silicone gel is effective in preventing and improving scars formed due to a wound formation after injury. OBJECTIVES: This study investigates whether a silicone gel composition based on a novel concept of infusing a biologically active material such as hyaluronic acid and/or salts with various polysiloxane derivatives in a specific proportion to achieve desired viscosity range and their action has a synergistic beneficial effect on skin scar after injury. METHODS: We have developed a topical gel utilizing a combination of emulsifiers, sodium hyaluronate, polysiloxane, and its derivatives. The method of preparation comprises mixing of aqueous phase dispersion and polysiloxanes blend under stirring at room temperature. RESULTS: It results in the formation of a homogenous smooth gel formulation. The developed topical gel formulation was characterized for physicochemical properties, rheology, stability, and anti-scar activity in Wistar rats. It was found that the developed formulation system consists of desirable attributes for skin applications. In vivo investigation of developed polysiloxane gel formulation for anti-scar activity shown promising outcomes compared to marketed product (Kelo-cote scar gel). Furthermore, a histopathology study of healed skin tissues observed the formation of microscopic skin structures compared to the Kelo-cote scar gel. CONCLUSIONS: It indicates that the combination of polysiloxanes and sodium hyaluronate resulting an improvement in anti-scar activity compared to the marketed product containing polysiloxanes alone.


Asunto(s)
Cicatriz , Ácido Hialurónico , Geles de Silicona , Siloxanos , Animales , Ratas , Administración Tópica , Cicatriz/tratamiento farmacológico , Cicatriz/etiología , Cicatriz/patología , Cicatriz/prevención & control , Geles/administración & dosificación , Geles/química , Ácido Hialurónico/administración & dosificación , Ratas Wistar , Geles de Silicona/administración & dosificación , Geles de Silicona/química , Siloxanos/administración & dosificación , Viscosidad , Combinación de Medicamentos , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/química , Piel/efectos de los fármacos , Piel/patología
17.
J Diabetes Metab Disord ; 22(1): 119-133, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-37255773

RESUMEN

Objectives: The objective of the present study is to discuss the use of nanomaterials like nanosensors for diagnosing Diabetes and highlight their applications in the treatment of Diabetes. Methods: Diabetes mellitus (D.M.) is a group of metabolic diseases characterized by hyperglycemia. Orally administered antidiabetic drugs like glibenclamide, glipalamide, and metformin can partially lower blood sugar levels, but long-term use causes kidney and liver damage. Recent breakthroughs in nanotheranostics have emerged as a powerful tool for diabetes treatment and diagnosis. Results: Nanotheranostics is a rapidly developing area that can revolutionize diabetes diagnosis and treatment by combining therapy and imaging in a single probe, allowing for pancreas-specific drug and insulin delivery. Nanotheranostic in Diabetes research has facilitated the development of improved glucose monitoring and insulin administration modalities, which promise to improve the quality of life for people with Diabetes drastically. Further, nanomaterials like nanocarriers and unique functional nanomaterials used as nano theranostics tools for treating Diabetes will also be highlighted. Conclusion: The nanosensors discussed in this review article will encourage researchers to develop innovative nanomaterials with novel functionalities and properties for diabetes detection and treatment.

18.
J Biomol Struct Dyn ; : 1-12, 2023 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-38116764

RESUMEN

Within the realm of soluble factors that have emerged as potential targets for therapeutic intervention, the chemokine interleukin-8 (IL-8) has garnered attention as a potential contributor to treatment responses in various cancer types. The utilization of naturally occurring anticancer compounds for treating cancer patients has shown substantial advancements in survival rates across early and advanced stages of the disease. In silico research findings provide support for the application of phytochemicals as potential inhibitors of IL-8, and phytochemicals exhibiting a high binding free energy and crucial interactions display promising anticancer properties, positioning them as candidates for future drug development. Noteworthy phytochemicals such as IMPHY006634 (Isohydnocarpin), IMPHY007957 (Chitranone) and IMPHY013015 (1-Hydroxyrutaecarpine) were predicted to possess inhibitory activity against IL-8, with calculated energies ranging from -9.9 to -9.1 kcal/mol, respectively. Several hydrogen bonds, including common amino acid residues Lys9 and CYS48, were identified. Molecular dynamics calculations conducted on these potent inhibitors demonstrated their stability throughout a 200 ns simulation, as indicated by metrics such as RMSD, RMSF, Rg, SASA, H-bonds, PCA and FEL analysis. Moreover, PASS analysis and adherence of these natural compounds to drug-likeness rules like Lipinski's further strengthen their candidacy. Considering these calculations and various parameters, these three prominent natural compounds emerge as promising candidates for anti-IL-8 therapy in the management of cancer.Communicated by Ramaswamy H. Sarma.

19.
Mol Pharm ; 9(11): 2986-94, 2012 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-22994847

RESUMEN

The aim of this study was to develop novel colon targeted mucoadhesive microspheres (MAMs) for site specific delivery of 5-fluorouracil (5-FU) to colon without the drug being released in the stomach or small intestine. MAMs were prepared using Assam Bora rice starch, a natural mucoadhesive polymer, by a double emulsion solvent evaporation method. The microspheres were characterized for their shape, size, surface morphology, size distribution, incorporation efficiency, and in vitro and in vivo drug release studies. The release study confirmed the insignificant release of 5-FU in physiological condition of stomach and small intestine and major drug release in the cecal content. In vivo release study of the optimized MAMs was compared with immediate release (IR) 5-FU. 5-FU was distributed predominantly in the upper GI tract from the IR, whereas 5-FU was distributed primarily to the lower part of the GI tract from the MAM formulation. Enhanced levels of liver enzymes were found in animals given IR 5-FU as well as augmented levels of serum albumin, creatinine, leucocytopenia and thrombocytopenia was also observed. Thus to sum up, it can be appropriately established that the 5-FU release pattern from MAMs exhibits slow and extended release over longer periods of time with reduced systemic side effects.


Asunto(s)
Neoplasias Colorrectales/tratamiento farmacológico , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Fluorouracilo/administración & dosificación , Microesferas , Oryza/química , Almidón/administración & dosificación , Adhesividad , Animales , Antimetabolitos Antineoplásicos/administración & dosificación , Antimetabolitos Antineoplásicos/sangre , Antimetabolitos Antineoplásicos/farmacocinética , Materiales Biocompatibles Revestidos/química , Neoplasias Colorrectales/metabolismo , Neoplasias Colorrectales/patología , Portadores de Fármacos/farmacocinética , Fluorouracilo/sangre , Fluorouracilo/farmacocinética , Tracto Gastrointestinal/efectos de los fármacos , Cabras , Masculino , Tamaño de la Partícula , Ratas , Almidón/farmacocinética , Distribución Tisular
20.
Drug Dev Ind Pharm ; 38(1): 84-92, 2012 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-21726136

RESUMEN

Encapsulation of Ganciclovir in lipophilic vesicular structure may be expected to enhance the oral absorption and prolong the existence of the drug in the systemic circulation. So the purpose of the present study was to improve the oral bioavailability of Ganciclovir by preparing nanosized niosomal dispersion. Niosomes were prepared from Span40, Span60, and Cholesterol in the molar ratio of 1:1, 2:1, 3:1, and 3:2 using reverse evaporation method. The developed niosomal dispersions were characterized for entrapment efficiency, size, shape, in vitro drug release, release kinetic study, and in vivo performance. Optimized formulation (NG8; Span60:Cholesterol 3:2 molar ratio) has shown a significantly high encapsulation of Ganciclovir (89±2.13%) with vesicle size of 144±3.47 nm (polydispersity index [PDI]=0.08). The in vitro release study signifies sustained release profile of niosomal dispersions. Release profile of prepared formulations have shown that more than 85.2±0.015% drug was released in 24 h with zero-order release kinetics. The results obtained also revealed that the types of surfactant and Cholesterol content ratio altered the entrapment efficiency, size, and drug release rate from niosomes. In vivo study on rats reveals five-time increment in bioavailability of Ganciclovir after oral administration of optimized formulation (NG8) as compared with tablet. The effective drug concentration (>0.69 µg/mL in plasma) was also maintained for at least 8 h on administration of the niosomal formulation. In conclusion, niosomes can be proposed as a potential oral delivery system for the effective delivery of Ganciclovir.


Asunto(s)
Portadores de Fármacos/química , Ganciclovir/administración & dosificación , Ganciclovir/química , Liposomas/química , Nanopartículas/química , Administración Oral , Animales , Disponibilidad Biológica , Química Farmacéutica , Colesterol/química , Preparaciones de Acción Retardada , Sistemas de Liberación de Medicamentos/métodos , Tamaño de la Partícula , Farmacocinética , Ratas , Tensoactivos/química , Temperatura de Transición
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