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1.
J Microencapsul ; : 1-15, 2024 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-38780157

RESUMO

AIM: The present work is focus on development of anti-psoriasis activity of Karanjin (isolated from Pongamia pinnata seed oil) loaded liposome based lotion for enhancement of skin permeation and retention. METHOD: Karanjin was isolated using liquid-liquid extraction method and characterised by HPLC analysis and partition coefficient. Further, isolated Karanjin was loaded into liposomes using thin-film hydration technique and optimised by Box-Behnken design. Selected optimised batch was characterised their mean diameter, PDI, zeta potential, and entrapment efficiency, morphology (by TEM), FTIR and ex-vivo skin retention. Additionally, Karanjin loaded liposomes were formulated into lotion and characterise their rheological, spreadability, texture, ex-vivo skin permeation & retention, stability and anti-psoriatic activity in mouse tail model. RESULT: The yield of Karanjin from seed oil was 0.1% w/v and have lipophilic nature. The optimised liposomal formulation showed 195 ± 1.8 nm mean diameter, 0.271 ± 0.02 PDI, -27.0 ± 2.1 mV zeta potential and 61.97 ± 2.5% EE. TEM image revel the spherical shap of liposome surrounded by single phospholipid bilayer and no interection between drug and excipients. Further, lotion was prepared by 0.1% w/v carbopol and found to 615 mPa.sec viscosity, good thixotropic behaviour, spreadability and texture. There was 22.44% increase in drug permeation for Karanjin loaded liposomal lotion compared to pure Karanjin lotion, confirm by ex-vivo permeation and retention. While, in-vivo study revel the liposomal lotion of Karanjin was found to have 16.09% higher drug activity then 5% w/w conventional Karanjin lotion. CONCLUSION: Karanjin loaded liposomal lotion have an effective anti-psoriatic agent and showed better skin permeation and retention than the conventional Karanjin lotion.

2.
Ther Deliv ; 15(3): 181-192, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38356357

RESUMO

Aim: Optimization and evaluation of Aceclofenac nanoemulgel for treatment for rheumatoid arthritis and reduction of GI irritation and enhancement of bioavaibility. Materials & methods: Different batches of emulgel and selected batch was proceeded for characterization like particle size, scanning electron microscopy, drug ingredient, in vitro release, Fourier transform infrared and x-ray diffraction in vitro inflammation and gel evaluation such as (spreadability, swelling index), ex vitro permeation, skin irritation and in vivo anti-inflammatory. Result: Emulgel showed nanometri size sustained release (79.96% in 6 h), compatibility and anti-inflammatory activity compared with pure drug. Concluded that emulgels had better (nearly twice as good) anti-inflammatory action as the commercial product. Conclusion: Compared with the commercial gel, the emulgel's anti-inflammatory effect had a quicker onset and a longer duration of action.


A non-steroidal anti-inflammatory drug (NSAID) aceclofenac is used as the treatment for rheumatoid arthritis. It is generally taken orally. However, there are a few issues with it being taken this way. The main ones are: some of the drug reacts too early in the body, meaning only a small amount of it reaches the parts of the body where it is needed; it can irritate the digestive system; and it does not dissolve very well in water, which also makes it harder to reach the parts of the body where it is needed. The authors of this study created a new type of gel for people to rub into their skin, instead of taking a pill. They hoped that this would allow the drug to be absorbed more directly into the parts of the body where it was needed, without irritating the digestive system. They tested the gel to see how well it contained and released the drug, how well it absorbed into the skin, and whether it irritated the skin. They found that the gel contained and released the drug more effectively than similar gels which are already available and caused less irritation to the skin.


Assuntos
Anti-Inflamatórios não Esteroides , Osteoartrite , Humanos , Anti-Inflamatórios não Esteroides/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Inflamação/tratamento farmacológico , Osteoartrite/tratamento farmacológico , Géis
3.
Chem Biodivers ; 21(3): e202301468, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38206170

RESUMO

INTRODUCTION: Cancer poses a significant public health challenge in both developed and developing nations, with a rising global incidence of patients facing the threat of death due to abnormal cell proliferation. AIM: Review explores the utilization of different parts of herbal medicinal plants and their active pharmaceutical constituents in the prevention and treatment of various types of cancer. METHODOLOGY: Various anticancer medicinal plants have been identified, demonstrating their therapeutic effects by inhibiting cancer-stimulating enzymes and hormones, activating DNA repair processes, boosting the synthesis of protective stimulants, reducing the formation of free radicals, and enhancing individual immunity. Data for this study were gathered from diverse online bibliographic and databases, including Google, Google Scholar, Mendeley, Springer Link, Research Gate, and PubMed. RESULT: Herbal drugs have a huge contribution to the inhibition of the progression of cancer.A large volume of clinical studies has reported the beneficial effects of herbal medicines on the survival, immune modulation, and quality of life (QOL) of cancer patients, when these herbal medicines are used in combination with conventional therapeutics. CONCLUSION: The latest medicines for the clinical purpose (Above 50 %) are derived from herbal products. Furthermore, combination of these herbs with nanotechnology shows promise in treating specific carcinomas.


Assuntos
Neoplasias , Plantas Medicinais , Humanos , Medicina Herbária , Qualidade de Vida , Fitoterapia , Neoplasias/tratamento farmacológico , Preparações Farmacêuticas , Extratos Vegetais/uso terapêutico
4.
Curr Pharm Des ; 29(44): 3519-3531, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38111114

RESUMO

Contemporary medical research increasingly focuses on the blood-brain barrier (BBB) to maintain homeostasis in healthy individuals and provide solutions for neurological disorders, including brain cancer. Specialized in vitro modules replicate the BBB's complex structure and signalling using micro-engineered perfusion devices and advanced 3D cell cultures, thus advancing the understanding of neuropharmacology. This research explores nanoparticle-based biomolecular engineering for precise control, targeting, and transport of theranostic payloads across the BBB using nanorobots. The review summarizes case studies on delivering therapeutics for brain tumors and neurological disorders, such as Alzheimer's, Parkinson's, and multiple sclerosis. It also examines the advantages and disadvantages of nano-robotics. In conclusion, integrating machine learning and AI with robotics aims to develop safe nanorobots capable of interacting with the BBB without adverse effects. This comprehensive review is valuable for extensive analysis and is of great significance to healthcare professionals, engineers specializing in robotics, chemists, and bioengineers involved in pharmaceutical development and neurological research, emphasizing transdisciplinary approaches.


Assuntos
Inteligência Artificial , Neoplasias Encefálicas , Humanos , Encéfalo , Barreira Hematoencefálica , Sistemas de Liberação de Medicamentos
5.
J Microencapsul ; 40(8): 599-612, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37787159

RESUMO

AIM: The goal of this study is to optimisation and evaluation of dopamine-loaded NLC (NLC-DOPA) for achieve dopamine concentrations into brain for treatment of Parkinson's disease which causes progressive neuronal death. METHOD: NLC-DOPA prepared by homogenisation method using solid lipids (Cholesterol and Soya lecithin), liquid lipid (Oleic acid) and surfactant (Poloxamer- 188) as major excipients, optimised by central composite design using design expert-13 software. The optimised formulations were characterised by particle size, zeta potential, entrapment efficiency, SEM, TEM, FTIR, DSC, XRD, stability study and in-vitro drug release. The histopathology of rat brain tissues and goat nasal tissues were performed. The ex-vivo (permeability and nasal ciliotoxicity study) and in vivo pharmacodynamics study were also accomplished to determine its efficacy and potency of NLC. RESULT: The NLC-DOPA formulations were optimised in particle size and (EE)% with range from 85.53 ± 0.703 to 106.11 ± 0.822 nm and 82.17 ± 0.794 to 95.45 ± 0.891%, respectively. The optimised formulation F11 showing best goodness-fitted model kinetic, followed by Korsmeyer-Peppas equation and zero order kinetic. The SEM and TEM confirmed the spherical and smooth morphology of formulation. FTIR and DSC spectra were given compatibility of compound and XRD diffractograms confirmed the amorphous nature. An ex-vivo study was showed the high permeability coefficient (6.67*1 0 -4 cm/min, which is twice, compare to pure drug) and there was no damage in nasal mucosa, confirmed by the ciliotoxicity study. In-vivo study was shown significant effects of optimised NLC-DOPA on locomotor activity, force-swimming test and neurochemical assessment using rotenone induced Parkinson's model on Albino Wistar rats. CONCLUSION: NLC-DOPA was prepared and optimised successfully with increased bioavailability of drug from the NLC into brain with reduce toxicity in effective treatment of Parkinson's disease.


Assuntos
Nanoestruturas , Doença de Parkinson , Ratos , Animais , Dopamina , Doença de Parkinson/tratamento farmacológico , Portadores de Fármacos/química , Lipídeos/química , Nanoestruturas/química , Ratos Wistar , Di-Hidroxifenilalanina , Tamanho da Partícula
6.
J Biomater Sci Polym Ed ; 34(8): 1053-1066, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-36469754

RESUMO

Berberine is an anticancer medication that generates side effects due to its hydrophobicity and low cellular promiscuity as well as high dose requirement. Thus, have to prepare PEGylated dendrimer conjugates which increases the targeting and release of chemotherapeutic drugs at the tumor site although falling the adverse side effects. The circulation time of drug is enhanced by PEGylation. It is the covalent attachment of PEG to therapeutic protein or any molecule. PEGylated berberine dendrimer was prepared by biotinylation cross linking method and characterized by particle size, zeta potential, entrapment efficiency, in vitro release and stability study. The Structure validation of berberine before and after grafting was confirmed by FTIR and NMR spectroscopy. Further prepared PEGylated complex were proceeded for the cellular uptake study in AMJ-13, and BT-20 cells line by fluorescent microscopy study and MTT assay cytotoxicity study in MCF-7 cell line. The prepared PEGylated formulation showed nanometric size, desired zeta potential, and 69.56 ± 23% entrapment efficiency. The prepared PEGylated particle showed 70.23% release at 72 h with good stability at 90 days. The cellular uptake of formulation was highly appreciable which is clearly observed in AMJ-13 and BT-20 cells line. In comparison to pure drug, developed formulation has 10.8 M high efficiency for breast cancer cell line. PEGylation is easy and reasonable way, as it requires lesser time and is proved to be superior technique for treatment of cancer.


Assuntos
Berberina , Dendrímeros , Humanos , Dendrímeros/química , Portadores de Fármacos/química , Polietilenoglicóis/química
7.
Curr Drug Targets ; 24(3): 261-273, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36475350

RESUMO

The mucosal surfaces are the key site of the entrance, protection, and stability of several pathogens. Considering that >90% of pathogens gain access to the body via mucosal sites, using mucosal vaccination to generate protective immunity at mucosal sites could overcome. Some of the micro and nano carrier-based nasal delivery systems produce cellular, humoral and mucosal immunity. The nasal route vaccination may protect multiple distant mucosal sites like-rectal, vaginal, oral, and pulmonary. Also, it is a convenient and cost-effective vaccination mode with improved patient compliance. Several nasal vaccine delivery systems are currently being supplied in the form of liposomes, micro/nano particulates, which have shown immunity in animal models. Especially particulate nanovaccine has a special character related to long-term immunogenicity and high efficiency. The significance and the ability of the nasal route vaccination programs are unexplained and complications; therefore, effective delivery strategies will promote the production of nasal vaccines. The present study focuses on vaccine delivery strategies and their effects on the immune system. Also, the study discusses the benefits of mucosal-associated immune response over the conventional delivery system for vaccine via the nasal route.


Assuntos
Vacinas , Animais , Feminino , Administração Intranasal , Sistemas de Liberação de Medicamentos , Vacinação , Imunidade nas Mucosas
8.
Recent Pat Nanotechnol ; 17(4): 359-377, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35986540

RESUMO

COVID-19, caused by the SARS-CoV-2 virus, has been expanding. SARS-CoV caused an outbreak in early 2000, while MERS-CoV had a similar expansion of illness in early 2010. Nanotechnology has been employed for nasal delivery of drugs to conquer a variety of challenges that emerge during mucosal administration. The role of nanotechnology is highly relevant to counter this "virus" nano enemy. This technique directs the safe and effective distribution of accessible therapeutic choices using tailored nanocarriers, as well as the interruption of virion assembly, by preventing the early contact of viral spike glycoprotein with host cell surface receptors. This study summarises what we know about earlier SARS-CoV and MERS-CoV illnesses, with the goal of better understanding the recently discovered SARS-CoV-2 virus. It also explains the progress made so far in creating COVID-19 vaccines/ treatments using existing methods. Furthermore, we studied nanotechnology- based vaccinations and therapeutic medications that are now undergoing clinical trials and other alternatives.


Assuntos
COVID-19 , Coronavírus da Síndrome Respiratória do Oriente Médio , Humanos , COVID-19/prevenção & controle , SARS-CoV-2 , Vacinas contra COVID-19/uso terapêutico , Nanotecnologia/métodos , Vacinação
9.
Curr Pharm Des ; 29(43): 3442-3457, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38270161

RESUMO

Coronavirus disease 2019 is a global pandemic, particularly affecting individuals with pre-existing lung conditions and potentially leading to pulmonary fibrosis. Age and healthcare system limitations further amplify susceptibility to both diseases, especially in low- and middle-income countries. The intricate relationship between Coronavirus disease 2019 and lung cancer highlights their clinical implications and the potential for early detection through biosensor techniques involving hedgehog and mucin signaling. This study highlights the connection between Coronavirus disease 2019 and lung cancer, focusing on the mucosa, angiotensin- altering enzyme 2 receptors, and their impact on the immune system. It details the inflammatory mechanisms triggered by Coronavirus disease 2019, which can result in pulmonary fibrosis and influence the cancer microenvironment. Various cytokines like Interleukins-6 and Tumor Necrosis Factor-alpha are examined for their roles in both diseases. Moreover, the review delves into the Hedgehog signaling pathways and their significance in lung cancer, particularly their influence on embryonic cell proliferation and tissue integrity. Mucin signaling is another vital aspect, highlighting the diverse mucin expression patterns in respiratory epithelial tissues and their potential as biomarkers. The review concludes with insights into diagnostic imaging techniques like chest computed tomography, Positron Emission Tomography and Computed Tomography, and Magnetic Resonance Imaging for early lung cancer detection, emphasizing the crucial role of biosensors in identifying specific biomarkers for early disease detection. This review provides a comprehensive overview of the clinical impact of Coronavirus disease 2019 on lung cancer patients and the potential for biosensors utilizing hedgehog and mucin signaling for early detection. It underscores the ongoing need for research and innovation to address these critical healthcare challenges.


Assuntos
COVID-19 , Neoplasias Pulmonares , Fibrose Pulmonar , Humanos , Proteínas Hedgehog , Mucinas , Neoplasias Pulmonares/diagnóstico , COVID-19/diagnóstico , Microambiente Tumoral
10.
J Microencapsul ; 39(6): 563-574, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36222429

RESUMO

BACKGROUND AND AIM: The study was to extend systemic circulation and biological half-life (t1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential. METHODS: RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability. RESULT: Prepared SLN showed 126.85 ± 12.09 nm particle size, -24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution. CONCLUSION: The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site.


Assuntos
Nanopartículas , Neoplasias da Próstata , Humanos , Masculino , Ratos , Animais , Resveratrol/farmacologia , Distribuição Tecidual , Lipídeos/farmacocinética , Neoplasias da Próstata/tratamento farmacológico , Tamanho da Partícula , Portadores de Fármacos/farmacocinética
11.
Curr Drug Targets ; 23(15): 1381-1405, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36065923

RESUMO

BACKGROUND: The pathogenesis of hepatic diseases involves several cells, which complicates the delivery of pharmaceutical agents. Many severe liver diseases affecting the worldwide population cannot be effectively treated. Major hindrances or challenges are natural physiological barriers and non-specific targeting of drugs administered, leading to inefficient treatment. Hence, there is an earnest need to look for novel therapeutic strategies to overcome these hindrances. A kind of literature has reported that drug safety and efficacy are incredibly raised when a drug is incorporated inside or attached to a polymeric material of either hydrophilic or lipophilic nature. This has driven the dynamic investigation for developing novel biodegradable materials, drug delivery carriers, target-specific drug delivery systems, and many other novel approaches. OBJECTIVE: Present review is devoted to summarizing receptor-based liver cell targeting using different modified novel synthetic drug delivery carriers. It also highlights recent progress in drug targeting to diseased liver mediated by various receptors, including asialoglycoprotein, mannose and galactose receptor, Fc receptor, low-density lipoprotein, glycyrrhetinic, and bile acid receptor. The essential consideration is given to treating liver cancer targeting using nanoparticulate systems, proteins, viral and non-viral vectors, homing peptides and gene delivery. CONCLUSION: Receptors based targeting approach is one such approach that was explored by researchers to develop novel formulations which can ensure site-specific drug delivery. Several receptors are on the surfaces of liver cells, which are highly overexpressed in various disease conditions. They all are helpful for the treatment of liver cancer.


Assuntos
Neoplasias Hepáticas , Nanopartículas , Humanos , Sistemas de Liberação de Medicamentos , Nanotecnologia , Portadores de Fármacos/química , Neoplasias Hepáticas/tratamento farmacológico , Nanopartículas/química
12.
Drug Dev Ind Pharm ; 48(1): 21-28, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35703403

RESUMO

Migraine is a frequent neurological condition characterized by throbbing headaches, nausea, photophobia, and phonophobia, among other symptoms. Sumatriptan belongs to a BCS class III, which exhibits poor oral bioavailability and several side-effects. The objective of the present study was to develop solid lipid nanoparticles (SLNPs) of sumatriptan succinate for brain targeting by nasal route. Solvent injection method was used to increase the entrapment efficiency of hydrophilic drug. Thus, formulation was optimized by central composite design with minimum particle size, optimized zeta potential, and maximum entrapment efficiency, which was found to be 133.4 nm, -17.7 mV, and 75.5%, respectively. Optimized batch was further evaluated for surface morphology, Fourier-transform infrared spectroscopy, in vitro release, permeation across nasal mucosa, and histopathology. It was seen that most of the particles were spherical in shape as confirmed by scanning electron microscopy and transmission electron microscopy. The release of drug through the lipid showed initial burst release followed by sustained release up to 12 h. The ex vivo diffusion study using goat nasal mucosa at pH 6.8 revealed that SLNPs permeation across nasal mucosa was quick, which was sufficient for brain targeting. Histopathology studies further revealed integrity of nasal mucosa after treatment with SLNPs. The investigation indicated that hydrophilic drug, sumatriptan succinate can be successfully entrapped in SLNPs to target brain via nasal delivery, and thus it could be an effective approach for nose-to-brain delivery.


Assuntos
Nanopartículas , Sumatriptana , Administração Intranasal , Encéfalo , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Lipossomos , Nanopartículas/química , Mucosa Nasal , Tamanho da Partícula , Polímeros , Sumatriptana/química , Sumatriptana/farmacologia
13.
J Microencapsul ; 39(4): 352-363, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35635238

RESUMO

AIM: The research focussed on development and evaluation of ethosome as an effective delivery of antigen that eliminates need for frequent dose of antigen while improving patient compliance for Hepatitis B. METHOD: Prepared a single dose HBsAg ethosomal vaccine using a cold method and applied a central composite design optimisation using particles size, zeta potential and entrapment efficiency as dependent variables. Further, selected batch was assessed for their morphology, in vitro release, interaction, haemocompatibility, histological (ex vivo skin permeation) and stability studies. Further, proceeded for in-vivo study, administered in BALB/c mice via nasal route to check the immunological activity and compared with single and multiple doses of ethosome to booster doses of alum-HBsAg vaccine. Immunological marker like immunoglobulin (IgG and IgA) and cytokines (interleukin-2 and interferon-Y) were measured by ELISA techniques. RESULTS: The prepared ethosome showed minimum particle size (93.98 ± 4.6), 15.0 ± 2.83 mV zeta potential, with maximum entrapment efficiency (66.25 ± 8.6%). Physicochemical characterisation reveal the sustained release, haemocampatibile, and stable nature of ethosome. Further, ex-vivo skin permeation showed safely administration of drug by nasal route without toxicity. The in vivo study, found the higher immunological response observed in BALB/c mice, compare to alum-HBsAg vaccine. The single dose of ethosome showed sufficient effective and measurable immunoglobulin and cytokines levels. CONCLUSION: A single dose of ethosome is sufficient for the complete immunological response not require booster administration. The potency of ethosomes have to produce a protective immune response, as well as their ability to explore and target the immunological environment through nasal route.


Assuntos
Antígenos de Superfície da Hepatite B , Hepatite B , Administração Intranasal , Animais , Hepatite B/prevenção & controle , Camundongos , Camundongos Endogâmicos BALB C , Pele
14.
J Microencapsul ; 39(4): 299-313, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35470755

RESUMO

AIM: The current study focussed on the development and evaluation of aqueous core nanocapsules (ACNs) as an effective carrier to deliver an optimal synergistic combination of a highly water-soluble Vinorelbine bitartrate (VRL) and a poorly water-soluble Resveratrol (RES) for treatment of breast cancer. METHODS: Various molar ratios of VRL to RES were screened against MCF-7 cell lines to determine the synergistic effects using the Chou-Talalay method. The synergistic ratio of therapeutic agents was then incorporated into aqueous core nanocapsules utilising a double emulsion solvent evaporation technique to yield dual drug-loaded nanocapsules (dd-ACNs). The dd-ACNs were optimised using Box-Behnken design and characterised for physicochemical parameters such as particle size, zeta potential, polydispersity index, total drug content and encapsulation efficiency, surface morphology, drug excipient compatibility by FTIR and DSC, release kinetics, toxicity studies and anticancer efficacy (in-vitro and in-vivo). RESULTS: Results demonstrated that the combination exhibited maximum synergy when higher doses of VRL were combined with smaller doses of RES (1:1, 5:1, and 10:1). The dual drug-loaded ACNs were found to be stable and depicted a core-shell structure, narrow size range (150.2 ± 3.2 nm) with enhanced encapsulation (80% for VRL and 99% for RES). Moreover, the dd-ACNs were 5 times more efficacious in-vitro than a combination of free drugs, while reducing systemic toxicity. Also, pre-clinical evaluation of dd-ACNs also depicted a drastic reduction of tumour volume as compared tp pristine VRL and a physical combination of drugs. CONCLUSION: The developed dd-ACNs can be applied as a potential carrier for delivery of a combination of chemotherapeutics at a synergistic ratio at the tumour site.


Assuntos
Neoplasias da Mama , Nanocápsulas , Neoplasias da Mama/tratamento farmacológico , Feminino , Humanos , Nanocápsulas/química , Polímeros , Resveratrol/farmacologia , Vinorelbina , Água/química
15.
J Microencapsul ; 39(2): 125-135, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35282781

RESUMO

AIM: This work studies the development and evaluation of Gymnema sylvestre (GYM) extract loaded sustained release polymeric nanoparticles (PNPs) for enhanced bioavailability and reduced nephrotoxicity. The current therapy is associated with the drawbacks of addiction and repeated administration. METHOD: The sustained release PNPs were developed and evaluated for toxicity. PNPs of GYM were prepared by double emulsion solvent evaporation technique utilising Taguchi model and evaluated for physicochemical properties (particle size, zeta potential, entrapment efficiency), in vitro drug release, compatibility, and stability. Further, the bioavailability and in vivo nephrotoxicity studies in diabetic rat model were also carried out. RESULT: The developed optimised nanoparticles were 205.7 ± 1.20 nm in size, -40.68 mV zeta potential, compatible, and stable in nature with improved entrapment efficiency (67.1 ± 0.2%) and sustained release. Moreover, nanoparticles were found to lower the blood glucose level in single as well as multiple doses. Results of in vivo study indicated that GYM-NPs increased the phosphorylase activity and thus enhanced insulin secretion. Furthermore, the nanoparticles were free from toxicity, which was confirmed by the estimation of kidney biomarker. CONCLUSION: The nanoparticles increased the bioavailability of GYM extract and have a great potential for the treatment of diabetes in reduced dose, and so these can be potential candidates for treating diabetes.


Assuntos
Gymnema sylvestre , Nanopartículas , Animais , Preparações de Ação Retardada/química , Portadores de Fármacos/química , Gymnema sylvestre/química , Nanopartículas/química , Tamanho da Partícula , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polímeros/química , Ratos
16.
J Biomater Sci Polym Ed ; 32(2): 266-280, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-32942961

RESUMO

PEGylation is the covalent addition of PEG to one more molecule. PEGylation can improve the maintenance time of the therapeutics similar to proteins, liposomes, and nanoparticle through shielding them beside different debasing mechanisms dynamic in a body that improve beneficial properties. This skill is used to get better half-life and other pharmaceutical properties of a protein, peptide, or non-peptide molecule. Polyethylene glycol is harmless, non-immunogenic, non-antigenic, and extremely soluble in water and FDA accepted polymer. It shows a significant role in drug delivery. A variety of PEG-based formulations are available in the market. This paper represents the benefits of PEGylation over non-PEGylated products. Now a day, PEGylation plays an important role in the drug delivery system. PEGylation increases the therapeutic potential of drugs.


Assuntos
Sistemas de Liberação de Medicamentos , Proteínas , Lipossomos , Peptídeos , Polietilenoglicóis
17.
Crit Rev Ther Drug Carrier Syst ; 37(2): 183-204, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32865905

RESUMO

Nanotechnology provides an excellent platform for the development of a new generation of vaccines. These are based on purified subunit proteins or polysaccharides, recombinant proteins, synthetic peptides, or nucleic acids. These types of vaccines may be insufficiently immunogenic, thus requiring adjuvants that augment their immunogenicity. Nanoparticles (NPs) can act as adjuvants for vaccines, hence they are referred to as a nano-adjuvant (NA). NPs can either encapsulate or adsorb the vaccine antigen or DNA in an appropriate formulation, thus increasing stability, cellular uptake, and immunogenicity. In addition, the biodistribution and systemic release of a vaccine can also be controlled by different NA formulations. This review provides an overview of the classification of NAs and also addresses factors influencing the stability, release, and immunogenicity of the formulated vaccine. A basic understanding of these factors enables a more rational design of NA formulations. Applications of NAs and key challenges in their formulation development are also discussed.


Assuntos
Adjuvantes Imunológicos/química , Portadores de Fármacos/química , Nanopartículas/química , Vacinas/administração & dosagem , Desenvolvimento de Medicamentos/métodos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Humanos , Imunogenicidade da Vacina , Nanomedicina/métodos , Distribuição Tecidual , Vacinas/imunologia , Vacinas/farmacocinética
18.
J Immunol Methods ; 481-482: 112791, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32387695

RESUMO

The surface of the mucosa is the biggest path through which pathogens enter the human body. We need an understanding of mucosal immune systems to use vaccines that generate protective mucosal and systemic immunity to regulate the outbreak of various infectious diseases. The better impact of the mucosal vaccine over traditional injectable vaccines are that not only do they induce efficient immune reactions to the mucosa but they are also comfortable in physical aspect & psychological aspect. The material of the vaccine includes pathogens antigens and adjuvants, which enable vaccination to be effective. Vaccines are classified into different criteria, including the used vaccine material and method of administration. Vaccines have traditionally been injected through a needle. However, as most of the pathogens first infect the mucosal surfaces, and growing interest is expressed in establishing protective immunity from the mucosa, which is accomplished through mucosal paths through vaccinosis. To improve the existing vaccines further, innovative strategies derived from interdisciplinary scientific research will need to develop new vaccine production, storage, and delivery systems. A distinctive & vast research and development platform has been set up for the growth of the next generation of mucosal vaccinations. The latest science and technological advancement in the areas of molecular biology, bio and chemical engineering, genome and system biology has provided accumulated understanding of the inborn and acquired multi-dimensional immune system. This review summarizes recent developments in the use of mucosal vaccines and their associated nanoadjuvants for the control of infectious diseases.


Assuntos
Sistemas de Liberação de Medicamentos , Imunidade nas Mucosas/imunologia , Vacinas/imunologia , Adjuvantes Imunológicos/administração & dosagem , Animais , Humanos , Vacinas/administração & dosagem
19.
J Pharm Sci ; 108(2): 851-859, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30053555

RESUMO

The objective of the present study was to develop polymeric nanoparticles (PNPs) of frovatriptan succinate for brain targeting by nasal route. Double emulsion method was used to increase the entrapment efficiency of hydrophilic drug, and formulation was optimized by central composite design to achieve critical quality attributes namely particle size, zeta potential, and entrapment efficiency. Optimized batch was evaluated for surface morphology, in vitro release, permeation across nasal mucosa, stability, histopathology, and brain tissue uptake study. Prepared PNPs were found to be smooth with particle size of 264.4 ± 0.04 nm, zeta potential -35.17 ± 0.07 mV, and 65.2 ± 0.06% entrapment efficiency. PNPs showed biphasic release pattern, initial burst release followed by sustained release up to 72 h. Ex vivo diffusion study using goat nasal mucosa at pH 6.8 revealed that PNPs permeation across nasal mucosa was about 3 times more than the pure drug solution, and quick delivery of PNPs in brain region was confirmed by fluorescence microscopic evaluation in male Wistar rats after intranasal administration. Histopathology studies further revealed integrity of nasal mucosa after treatment with PNPs. The investigation indicated that hydrophilic drug, frovatriptan succinate can be successfully entrapped in PNPs to target brain via nasal delivery, and thus it could be an effective approach for nose to brain delivery.


Assuntos
Encéfalo/metabolismo , Carbazóis/administração & dosagem , Sistemas de Liberação de Medicamentos , Nanopartículas/metabolismo , Agonistas do Receptor de Serotonina/administração & dosagem , Triptaminas/administração & dosagem , Administração Intranasal , Animais , Carbazóis/farmacocinética , Portadores de Fármacos/metabolismo , Liberação Controlada de Fármacos , Masculino , Polímeros/metabolismo , Ratos Wistar , Agonistas do Receptor de Serotonina/farmacocinética , Triptaminas/farmacocinética
20.
Curr Drug Deliv ; 15(9): 1284-1293, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30009708

RESUMO

BACKGROUND: Vinorelbine bitartrate (VRL) is an antimitotic agent approved by FDA for breast cancer and non-small cell lung cancer (NSCLC) in many countries. However, high aqueous solubility and thermo degradable nature of VRL limited the availability of marketed dosage forms. OBJECTIVES: The current work is focused on the development of lipid based aqueous core nanocapsules which can encapsulate the hydrophilic VRL in the aqueous core of nanocapsules protected with a lipidic shell which will further provide a sustained release. METHODS: The ACNs were prepared by double emulsification technique followed by solvent evaporation. Box Behnken Design was utilized to optimize the formulation and process variables. Thirteen batches were generated utilizing lipid concentration, surfactant concentration and homogenizer speed as dependent variables (at three levels) and particle size and encapsulation efficiency as critical quality attributes. The ACNs were characterized for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, morphology by Transmission Electron Microscopy (TEM) and in vitro release. The ACNs were further evaluated for safety against intravenous administration by haemocompatibility studies. RESULTS: Results demonstrated that lipidic nanocapsules enhanced the entrapment efficiency of VRL up to 78%. Transmission Electron Microscopy revealed spherical shape of ACNs with core-shell structure. The GMS-VRL-ACNs showed that release followed Korsemeyer peppas kinetics suggesting Fickian diffusion. Moreover, the compliance towards haemocompatibility studies depicted the safety of prepared nanocapsules against intravenous administration. CONCLUSION: ACNs were found to be promising in encapsulating high aqueous soluble anticancer drugs with enhanced entrapment and safety towards intravenous administration.


Assuntos
Lipídeos/química , Nanocápsulas/química , Tartaratos/química , Vimblastina/química , Administração Intravenosa , Difusão , Humanos , Interações Hidrofóbicas e Hidrofílicas , Tamanho da Partícula , Propriedades de Superfície , Tartaratos/administração & dosagem , Tartaratos/síntese química , Vimblastina/administração & dosagem , Vimblastina/síntese química , Água/química
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