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1.
Artigo em Inglês | MEDLINE | ID: mdl-38566386

RESUMO

Wound healing is crucial for maintaining skin integrity and preventing complications from external threats. Various plants, such as Achillea millefolium, Aloe vera, Curcuma longa, Calendula officinalis, Camellia sinensis, Azadirachta indica, and Plantago, have demonstrated wound healing capabilities and have been used in herbal medicine for wound care. NLCs are second-generation lipid nanoparticles, blending solid and liquid lipids to improve medication loading and limit leakage. NLCs have been used in various applications, including cosmeceuticals, chemotherapy, gene therapy, and brain targeting. Wound healing is divided into four stages: hemostasis, inflammatory response, proliferation, and remodeling. Factors such as age, gender, chronic disorders, and local agents like infections can affect recovery. These plants' antiinflammatory, antioxidant, and antibacterial activities have demonstrated potential in wound healing. Combining herbal medicinal plants and nanostructured lipid carriers (NLCs) can revolutionise wound treatment and improve overall healthcare outcomes.

2.
Adv Pharm Bull ; 14(1): 48-66, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38585451

RESUMO

Delivery and formulation of oral peptide and protein therapeutics have always been a challenge for the pharmaceutical industry. The oral bioavailability of peptide and protein therapeutics mainly relies on their gastrointestinal solubility and permeability which are affected by their poor membrane penetration, high molecular weight and proteolytic (chemical and enzymatic) degradation resulting in limited delivery and therapeutic efficacy. The present review article highlights the challenges and limitations of oral delivery of peptide and protein therapeutics focusing on the application, potential and importance of solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) as lipid-based drug delivery systems (LBDDSs) and their advantages and drawbacks. LBDDSs, due to their lipid-based matrix can encapsulate both lipophilic and hydrophilic drugs, and by reducing the first-pass effect and avoiding proteolytic degradation offer improved drug stability, dissolution rate, absorption, bioavailability and controlled drug release. Furthermore, their small size, high surface area and surface modification increase their mucosal adhesion, tissue-targeted distribution, physiological function and half-life. Properties such as simple preparation, high-scale manufacturing, biodegradability, biocompatibility, prolonged half-life, lower toxicity, lower adverse effects, lipid-based structure, higher drug encapsulation rate and various drug release profile compared to other similar carrier systems makes LBDDSs a promising drug delivery system (DDS). Nevertheless, undesired physicochemical features of peptide and protein drug development and discovery such as plasma stability, membrane permeability and circulation half-life remain a serious challenge which should be addressed in future.

3.
Nanomedicine (Lond) ; 2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38661720

RESUMO

Aim: To investigate the therapeutic potential of mebendazole (MBZ)-loaded nanostructured lipid carriers (NLCs). Methodology: NLC-MBZ was prepared and characterized to evaluate the in vitro and in vivo anticancer effects and the inhibitory effect on RanGTP and its potential as an antimetastatic treatment in vivo. Results: NLC-MBZ exhibited a size and charge of 155 ± 20 nm and -27 ± 0.5 mV, respectively, with 90.7% encapsulation. Free MBZ and NLC-MBZ had a 50% inhibitory concentration of 610 and 305 nM, respectively, against MDA-MB-231 cell lines. NLC-MBZ decreased tumor size, suppressed tumor lung metastases, and lowered the expression of CDC25A, SKP2, RbX1 and Cullin1 while boosting the Rb proteins. Conclusion: NLC-MBZ displayed antiangiogenic potential and resulted in a reduced rate of lung metastasis in vivo.

4.
Am J Cancer Res ; 14(3): 1101-1120, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38590403

RESUMO

Morellic acid (MA), a typical compound found in Garcinia plants, is known for its anticancer properties. In present study, we isolated MA from resin of Garcinia hanburyi Hook. f. using preparative chromatography. We have successfully prepared MA-loaded nanostructured lipid carriers (MA-NLCs) and refined the production process via orthogonal testing. Optimization of the preparation process resulted in an average particle size of 165.50±1.70 nm with a PDI of 0.19±0.01. The EE% and DL% of MA-NLCs were 78.17±0.34% and 7.25±0.38%, respectively. The zeta potential of MA-NLCs was -21.85±0.67 mV. Comparatively, MA-NLCs showed a greater area under the curve (AUC) and an extended half-life (t1/2) than free MA. Pharmacokinetics analysis revealed that the AUC0-t increased from 4.91±0.65 µg/mL∙min (free MA) to 18.91±3.40 µg/mL∙min (MA-NLCs) and the t1/2 value for MA-NLCs was 7.93-fold longer than that of free MA. In vitro cytotoxic assessments indicated that MA formulations curtailed the proliferation of cancer cells. In vivo, MA-NLCs significantly inhibited the tumor growth in tumor-bearing mouse model. Molecular mechanism studies revealed that up-regulation of apaf-1 and activation of caspase-3, caspase-9 and GSDME by MA-NLCs may trigger to apoptosis and pyroptosis in cancer cells. Consequently, our findings support the potential of NLCs as an effective MA delivery system for the clinical management of cancer.

5.
Gels ; 10(3)2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38534578

RESUMO

The objective of the present study was to develop and evaluate NLC-chitosan hydrogel beads for topical administration. The feasibility of the preparation technology was verified by investigating various formulation factors and the impact of chitosan hydrogel beads on the NLC. The encapsulation efficiency of NLC-chitosan hydrogel beads was above 95% in optimized process conditions. The physical characterization of the NLC-chitosan hydrogel beads showed that the NLC was distributed within the network of the chitosan hydrogel beads. Furthermore, the incorporation of NLC into the chitosan hydrogel beads was related to the electrostatic interaction between the surface of the NLC and chitosan, which influenced the lipid ordering degree of the NLC and contributed to the stability. The stability studies showed that the retention rate of quercetin in the NLC-chitosan hydrogel beads was 88.63 ± 2.57% after 10 months of storage under natural daylight. An in vitro permeation study showed that NLC-chitosan hydrogel beads exhibited superior ability in enhancing skin permeation by hydrophobic active ingredients compared to the NLC and significantly increased skin accumulation. These studies demonstrated that the use of NLC-chitosan hydrogel beads might be a promising strategy for the delivery of hydrophobic active ingredients in topical administration.

6.
Acta Parasitol ; 2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38489009

RESUMO

PURPOSE: Resistance and adverse consequences of albendazole (ABZ) in treating trichinellosis urged demand for secure and effective new drugs. The current study aimed to assess the effect of chitosan-coated lipid nano-combination with albendazole and miltefosine (MFS) in treating experimental murine trichinellosis and evaluating pathological and immunological changes of trichinellosis. MATERIALS AND METHODS: One hundred twenty Swiss albino mice were divided into six groups. Each group was subdivided into a and b subgroups based on the scarification time, which was 7- and 40-days post-infection (PI), respectively. The treatment efficacy was evaluated using parasitological, histopathological, serological (interleukin (IL)-12 and IL-4 serum levels), immunohistochemical (GATA3, glutathione peroxidase1 (GPX1) and caspase-3), and scanning electron microscopy (SEM) methods. RESULTS: The most effective drug was nanostructured lipid carriers (NLCs) loaded with ABZ (G5), which showed the most significant reduction in adults and larval count (100% and 92.39%, respectively). The greatest amelioration in histopathological changes was reported in G4 treated with MFS. GATA3 and caspase-3 were significantly reduced in all treated groups. GPX1 was significantly increased in G6 treated with MFS + NLCs. The highest degenerative effects on adults and larvae by SEM were documented in G6. CONCLUSION: Loading ABZ or MFS on chitosan-coated NLCs enhanced their efficacy against trichinellosis. Although ABZ was better than MFS, their combination should be considered as MFS caused a significant reduction in the intensity of infection. Furthermore, MFS showed anti-inflammatory (↓GATA3) and antiapoptotic effects (↓caspase-3), especially in the muscular phase. Also, when loaded with NLCS, it showed an antioxidant effect (↑GPX1).

7.
Food Res Int ; 182: 114148, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38519178

RESUMO

In this current study, the internal structure of nanostructured lipid carriers was modulated by phospholipids (lecithin PC, hydrogenated soybean phospholipid HPC) and solid lipids to achieve stable encapsulation of citral. The presence of high melting point HPC could construct α-crystalline type with more lattice defects and effectively inhibit ß-ization. The HPC group could maintain the particle size at 155.9-186.9 nm, the polydispersity index (PDI) at 0.182-0.321, the Zeta potential at -57.58 mV to -49.35 mV and the retention rate of citral at 91.33-98.49 % in the acidic environments of 2 mM and 20 mM hydrochloric acid solutions. The recrystallization index (RI) of NLC increased with the number of solid lipid ester bonds (from 3.57 % to 16.58 % in the PC group and from 0.82 % to 12.47 % in the HPC group). The results illustrated that the number of solid lipid ester bonds and the melting point of phospholipids affected crystallinity of the lipid matrix and thus the stability of encapsulated citral. Hydrogenated phospholipid with high melting points was more beneficial in stabilizing citral. The present study improved the acidic stability of citral and provided a new thought for the application of citral in acidic beverages.


Assuntos
Monoterpenos Acíclicos , Nanoestruturas , Fosfolipídeos , Portadores de Fármacos/química , Nanoestruturas/química , Ésteres
8.
AAPS PharmSciTech ; 25(3): 57, 2024 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-38472545

RESUMO

Psoriasis is a complex and persistent autoimmune skin disease. The present research focused on the therapeutic evaluation of betulin-loaded nanostructured lipid carriers (BE-NLCs) towards managing psoriasis. The BE-NLCs were synthesized using the emulsification cum solidification method, exhibiting a spherical shape with a particle size of 183.5±1.82nm and a narrow size distribution window (PDI: 0.142±0.05). A high zeta potential -38.64±0.05mV signifies the relative stability of the nano-dispersion system. BE-NLCs show a drug loading and entrapment efficiency of 47.35±3.25% and 87.8±7.86%, respectively. In vitro release study, BE NLCs show a cumulative percentage release of 90.667±5.507% over BE-sol (57.334±5.03%) and BD-oint (42±4.58%) for 720min. In an ex vivo 24-h permeation study, % cumulative amount permeated per cm2 was found to be 55.667±3.33% from BE-NLCs and 32.012±3.26% from BE-sol, demonstrating a better permeability of 21.66% when compared to the standard formulation BD-oint. The in vivo anti-psoriatic activity in the IMQ-induced model shows topical application of BE-sol, BE-NLCs, and BD-oint resulted in recovery rates of 56%, 82%, and 65%, respectively, based on PASI (Psoriasis Area and Severity Index) score. Notably, BE-NLCs demonstrated a more significant reduction in spleen mass, indicating attenuation of the local innate immune system in psoriatic mice. Reductions in TNF-α, IL-6, and IL-17 levels were observed in both BE-sol and BE-NLCs groups compared to the disease control (DC) group, with BE-NLCs exhibiting superior outcomes (74.05%, 44.76%, and 49.26% reduction, respectively). Soy lecithin and squalene-based NLCs could be better carrier system for the improvement of the therapeutic potential of BE towards management of psoriasis.


Assuntos
Ácido Betulínico , Nanoestruturas , Psoríase , Camundongos , Animais , Imiquimode/efeitos adversos , Portadores de Fármacos/uso terapêutico , Psoríase/tratamento farmacológico , Lipídeos , Tamanho da Partícula
9.
Pharmaceutics ; 16(3)2024 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-38543306

RESUMO

Capsaicin and curcumin, the active components of chili and turmeric, are prone to instability when exposed to light. Therefore, this research aimed to enhance the photostability of both extracts via the use of antioxidants, natural sunscreen, and nanostructured lipid carriers (NLCs). NLCs were chosen for this this study due to their advantages in terms of stability, drug loading capacity, occlusive effect, skin penetration, and controlled release. The photostability of each extract and extracts mixed with antioxidants, including grape seed extract, tea extract, and chlorogenic acid, were determined. Chlorogenic acid can enhance the photostability of capsaicin from 6.79 h to 16.50 h, while the photostability of curcumin increased from 9.63 h to 19.25 h. In addition, the use of natural sunscreen (sunflower oil) also increased the photostability of capsaicin and curcumin. The mixed extracts were then loaded into NLCs. The particle size of the formulation was 153.73 nm with a PDI value of 0.25. It exhibited high entrapment efficiency (more than 95%). In addition, it effectively reduced the decomposition of capsaicin and curcumin. Importantly, the natural stabilizers chosen for NLC fabrication significantly improved the photostability of curcumin and capsaicin by 600% and 567% compared to the unstabilized counterparts. This improvement contributes to the sustainability and bioavailability of these compounds in both cosmeceutical and pharmaceutical products.

10.
Int J Pharm ; 657: 124048, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38537925

RESUMO

Doxorubicin hydrochloride (DOX) is an anticancer agent used in cancer chemotherapy. The purpose of this study was to design nanostructured lipid carriers (NLCs) of DOX as smart chemotherapy to improve its photostability and anticancer efficacy. The characteristics of DOX and DOX-loaded NLCs were investigated using UV-Vis spectroscopy, Fourier transform infrared (FTIR) spectroscopy, particle size, and zeta potential study. The cytotoxicity of DOX was evaluated against three cancer cell lines (HeLa, A549, and CT-26). The particle size and zeta potential were in the range 58.45-94.08 nm and -5.80 mV - -18.27 mV, respectively. The chemical interactions, particularly hydrogen bonding and van der Waals forces, between DOX and the main components of NLCs was confirmed by FTIR. NLCs showed the sustained release profile of DOX. The photostability results revealed that the NLC system improved the photostability of DOX. Cytotoxicity results using the three cell lines showed that all formulations improved the anticancer efficacy of free DOX, and the efficacy was dependent on cell type and particle size. These results suggest that DOX-loaded NLCs are promising chemotherapeutic agents for cancer treatment.

11.
Curr Alzheimer Res ; 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38445703

RESUMO

BACKGROUND: Alzheimer's Disease (AD) is a long-term brain disorder that worsens over time. A cholinesterase inhibitor called Donepezil HCl (DNZ) is used to treat and control AD. Due to its failure to reach the appropriate concentration in the brain cells, its efficacy upon oral administration is limited, and thus investigation of alternative administration route is necessary. OBJECTIVE: The objective of this study was to develop donepezil HCl-loaded Nanostructured Lipid Carriers (NLCs) that can bypass the blood-brain barrier and thus be directly delivered to the brain through the nasal route. This method improves availability at the site of action, reduces the negative effects of oral medication, and ensures an expedited commencement of action. METHOD: High-pressure homogenization and ultrasonication were used to formulate NLCs. Glyceryl Monostearate (GMS) as a solid lipid, Tween 80 as a surfactant, and Poloxamer 407 as a co-- surfactant were used. In this study, argan oil was employed as a liquid lipid as well as a penetration enhancer. RESULTS: The chosen NLCs displayed a particle size of 137.34 ± 0.79 nm, a PDI of 0.365 ± 0.03, and a zeta potential of -10.4 mV. The selected formulation showed an entrapment efficiency of 84.05 ± 1.30% and a drug content of 77.02 ± 0.23%. The concentration of the drug in the brain after intravenous and intranasal administration of DNZ NLCs at 1 h was found to be 0.490 ± 0.007 and 4.287 ± 0.115, respectively. Thus, the concentration of DNZ achieved in the brain after intranasal administration of DNZ NLCs was approximately 9 times more than the concentration when administered by intravenous route. CONCLUSION: The DNZ-loaded NLCs, when administered via nasal route, showed markedly improved drug availability in the brain, suggesting an efficient drug delivery strategy to treat Alzheimer's disease.

12.
Pharmaceutics ; 16(2)2024 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-38399304

RESUMO

The objective of this study was to develop a versatile lipid core for the 'brick-dust type of drugs' (poorly water-soluble and poorly lipid-soluble drugs). In the first step, excipients of different polarities were classified according to their behavior in aqueous solutions. Subsequently, binary mixtures were prepared with cetyl palmitate (Crodamol™ CP pharma, Campinas, São Paulo, Brazil) as the solid lipid, and its miscibility with other excipients was evaluated using Raman mapping and classical least squares (CLS). Based on the results, the excipients Crodamol™ CP pharma (hydrophobic), Super Refined™ DMI (dimethyl isosorbide; hydrophilic, Mill Hall, PA, USA), and Super Refined™ Lauryl Lactate (lauryl lactate, medium polarity, Mill Hall, PA, USA) were chosen to compose the lipid core. The ideal proportion of these excipients was determined using a mixture design and the standard deviation (STD) of image histograms as the response variables. After statistical evaluation of the DoE results, the final composition was determined, and drugs with different logP (0 to 10) and physicochemical characteristics were evaluated in the optimized mixture. The drugs butamben (Sigma-Aldrich Co., Spruce Street, St. Louis, MO, USA), tacrolimus (NutriFarm, São Paulo, Brazil), atorvastatin calcium, and resveratrol (Botica da Terra, Campinas, Brazil) presented a homogeneous distribution in the optimized lipid core, indicating that this is a promising system to be used in nanostructured lipid carrier (NLC) formulations of such types of drugs.

13.
AAPS PharmSciTech ; 25(3): 47, 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38424367

RESUMO

Lung cancer is one of the most severe lethal malignancies, with approximately 1.6 million deaths every year. Lung cancer can be broadly categorised into small and non-small-cell lung cancer. The traditional chemotherapy is nonspecific, destroys healthy cells and produces systemic toxicity; targeted inhalation drug delivery in conjunction with nanoformulations has piqued interest as an approach for improving chemotherapeutic drug activity in the treatment of lung cancer. Our aim is to discuss the impact of polymer and lipid-based nanocarriers (polymeric nanoparticles, liposomes, niosomes, nanostructured lipid carriers, etc.) to treat lung cancer via the inhalational route of drug administration. This review also highlights the clinical studies, patent reports and latest investigations related to lung cancer treatment through the pulmonary route. In accordance with the PRISMA guideline, a systematic literature search was carried out for published works between 2005 and 2023. The keywords used were lung cancer, pulmonary delivery, inhalational drug delivery, liposomes in lung cancer, nanotechnology in lung cancer, etc. Several articles were searched, screened, reviewed and included. The analysis demonstrated the potential of polymer and lipid-based nanocarriers to improve the entrapment of drugs, sustained release, enhanced permeability, targeted drug delivery and retention impact in lung tissues. Patents and clinical observations further strengthen the translational potential of these carrier systems for human use in lung cancer. This systematic review demonstrated the potential of pulmonary (inhalational) drug delivery approaches based on nanocarriers for lung cancer therapy.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Nanopartículas , Humanos , Lipossomos/uso terapêutico , Neoplasias Pulmonares/tratamento farmacológico , Portadores de Fármacos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Pulmão , Polímeros/uso terapêutico , Lipídeos
14.
J Nanobiotechnology ; 22(1): 50, 2024 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-38317220

RESUMO

Obesity is a major risk to human health. Adipogenesis is blocked by α-tocopherol and conjugated linoleic acid (CLA). However, their effect at preventing obesity is uncertain. The effectiveness of the bioactive agents is associated with their delivery method. Herein, we designed CLA-loaded tocol nanostructured lipid carriers (NLCs) for enhancing the anti-adipogenic activity of α-tocopherol and CLA. Adipogenesis inhibition by the nanocarriers was examined using an in vitro adipocyte model and an in vivo rat model fed a high fat diet (HFD). The targeting of the tocol NLCs into adipocytes and adipose tissues were also investigated. A synergistic anti-adipogenesis effect was observed for the combination of free α-tocopherol and CLA. Nanoparticles with different amounts of solid lipid were developed with an average size of 121‒151 nm. The NLCs with the smallest size (121 nm) showed greater adipocyte internalization and differentiation prevention than the larger size. The small-sized NLCs promoted CLA delivery into adipocytes by 5.5-fold as compared to free control. The nanocarriers reduced fat accumulation in adipocytes by counteracting the expression of the adipogenic transcription factors peroxisome proliferator activated receptor (PPAR)γ and CCAAT/enhancer-binding protein (C/EBP)α, and lipogenic enzymes acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS). Localized administration of CLA-loaded tocol NLCs significantly reduced body weight, total cholesterol, and liver damage indicators in obese rats. The biodistribution study demonstrated that the nanoparticles mainly accumulated in liver and adipose tissues. The NLCs decreased adipocyte hypertrophy and cytokine overexpression in the groin and epididymis to a greater degree than the combination of free α-tocopherol and CLA. In conclusion, the lipid-based nanocarriers were verified to inhibit adipogenesis in an efficient and safe way.


Assuntos
Adipogenia , Ácidos Linoleicos Conjugados , Tocoferóis , Masculino , Humanos , Ratos , Animais , Ácidos Linoleicos Conjugados/farmacologia , Ácidos Linoleicos Conjugados/metabolismo , alfa-Tocoferol/metabolismo , alfa-Tocoferol/farmacologia , Distribuição Tecidual , Obesidade/metabolismo , Adipócitos/metabolismo , Tecido Adiposo/metabolismo , Fígado/metabolismo
15.
Curr Drug Deliv ; 2024 01 10.
Artigo em Inglês | MEDLINE | ID: mdl-38213159

RESUMO

BACKGROUND: Gestational diabetes mellitus (GDM) poses significant risks during pregnancy for both mother and fetus. Adherence to oral antidiabetic medications, like glibenclamide (GB), can be challenging, necessitating novel drug delivery methods. Nanostructured lipid carriers (NLC) offer a promising approach by efficiently permeating the skin due to their small size and lipid-based composition. OBJECTIVE: This study aimed to develop and evaluate transdermal patches loaded with glibenclamide NLCs to treat GDM. METHODS: Glibenclamide NLCs were prepared using hot homogenization with ultrasonication and melt dispersion method. A central composite design was utilized to optimize the formulations. Transdermal patches containing optimized NLCs were developed using HPMC K 100 and Eudragit L polymers. The patches were evaluated for various parameters, and their pharmacokinetic and pharmacodynamic studies were carried out to assess their safety and efficacy. RESULTS: Optimized NLCs efficiently permeated rat skin. Cell viability studies indicated the non- toxicity of the formulations. NLC-loaded transdermal patches (F2 and F7) showed drug release of 1098 µg/cm2 and 1001.83 µg/cm2 in 24 h, with a 2.5-fold higher flux and permeation coefficient than the GB patch. Pharmacokinetic analysis revealed Tmax of 8 and 10 h and Cmax of 7127 ng/ml and 7960 ng/ml for F2 and F7, respectively, ensuring sustained drug action. AUC0-α was 625681 ng/ml·h and 363625 ng/ml·h for F2 and F7, respectively, indicating improved bioavailability. CONCLUSION: Transdermal patches incorporating NLCs hold promise for enhancing glibenclamide's therapeutic efficacy in GDM treatment. Improved skin permeation, sustained drug release, and enhanced bioavailability make NLC-based transdermal patches a potential alternative with better patient compliance.

16.
Nanotechnology ; 35(15)2024 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-38194705

RESUMO

Epilepsy is one of the most prevalent chronic neurological disorders characterized by frequent unprovoked epileptic seizures. Epileptic seizures can develop from a broad range of underlying abnormalities such as tumours, strokes, infections, traumatic brain injury, developmental abnormalities, autoimmune diseases, and genetic predispositions. Sometimes epilepsy is not easily diagnosed and treated due to the large diversity of symptoms. Undiagnosed and untreated seizures deteriorate over time, impair cognition, lead to injuries, and can sometimes result in death. This review gives details about epilepsy, its classification on the basis of International League Against Epilepsy, current therapeutics which are presently offered for the treatment of epilepsy. Despite of the fact that more than 30 different anti-epileptic medication and antiseizure drugs are available, large number of epileptic patients fail to attain prolonged seizure independence. Poor onsite bioavailability of drugs due to blood brain barrier poses a major challenge in drug delivery to brain. The present review covers the limitations with the state-of-the-art strategies for managing seizures and emphasizes the role of nanotechnology in overcoming these issues. Various nano-carriers like polymeric nanoparticles, dendrimers, lipidic nanoparticles such as solid lipid nanoparticles, nano-lipid carriers, have been explored for the delivery of anti-epileptic drugs to brain using oral and intranasal routes. Nano-carries protect the encapsulated drugs from degradation and provide a platform to deliver controlled release over prolonged periods, improved permeability and bioavailability at the site of action. The review also emphasises in details about the role of neuropeptides for the treatment of epilepsy.


Assuntos
Epilepsia , Humanos , Epilepsia/tratamento farmacológico , Epilepsia/metabolismo , Convulsões/tratamento farmacológico , Convulsões/metabolismo , Anticonvulsivantes/metabolismo , Anticonvulsivantes/uso terapêutico , Encéfalo/metabolismo , Nanotecnologia
17.
Recent Pat Nanotechnol ; 18(2): 179-189, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38197417

RESUMO

One of the drug delivery technologies is nanostructured lipid carriers (NLCs), which improve drug permeability and thus bioavailability. NLCs are nanoparticles made from a lipid matrix made up of a mixture of solid and liquid lipids. The inclusion of liquid lipids is useful in lowering the ordered structure of solid lipids, increasing nanoparticle loading capacity, and drug entrapment efficiency within NLCs. Hot homogenization, cold homogenization, micro-emulsion, emulsification-solvent diffusion, high shear homogenization, and/or ultrasonication techniques, double emulsion technique, melting dispersion method, membrane contractor technique, and evaporation solvent injection are some of the methods that can be used to make NLCs. Both hydrophilic and lipophilic medicines can be carried out by NLCs. They can deliver medications in a variety of ways, including oral, topical, transdermal, parenteral, and ophthalmic. During the process of preparing this review article, several distinct studies and patent reports about various methods of NLCs formulations, their various therapeutic applications, and various routes of administration were investigated and discussed. The study conducts an in-depth evaluation of the most recent research publications and patents. NLCs have been utilized to treat a variety of disorders, including cancer, fungal infections, bacterial infections, inflammation, liver diseases, and ocular infections, due to their benefits. They can deliver medications to specific locations throughout the body, allowing for drug targeting and a reduction in unwanted side effects. They can also be used to improve bioavailability, reduce the medication's supplied dose, and improve the drug's pharmacological activity.


Assuntos
Sistemas de Liberação de Medicamentos , Lipídeos , Emulsões , Patentes como Assunto , Solventes
18.
Int J Mol Sci ; 25(2)2024 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-38256029

RESUMO

In the present work, we demonstrate studies involving the influence of the formulation composition on the physicochemical properties of nanocarriers: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). Novel lipid-origin platforms were prepared using two "green" betaine-based surfactants, cocamidopropyl betaine (ROKAmina K30) and coco betaine (ROKAmina K30B), in combination with three different solid lipids, cetyl palmitate (CRODAMOL CP), trimyristin (Dynasan 114), and tristearin (Dynasan 118). Extensive optimization studies included the selection of the most appropriate lipid and surfactant concentration for effective SLN and NLC stabilization. The control parameters involving the hydrodynamic diameters of the obtained nanocarriers along with the size distribution (polydispersity index) were determined by dynamic light scattering (DLS), while shape and morphology were evaluated by atomic force microscopy (AFM) and transmission electron microscopy (TEM). Electrophoretic light scattering (ELS) and turbidimetric method (backscattering profiles) were used to assess colloidal stability. The studied results revealed that both betaine-stabilized SLN and NLC formulations containing CRODAMOL CP as lipid matrix are the most monodisperse and colloidally stable regardless of the other components and their concentrations used, indicating them as the most promising candidates for drug delivery nanosystems with a diverse range of potential uses.


Assuntos
Surfactantes Pulmonares , Tensoativos , Betaína , Sistemas de Liberação de Medicamentos , Difusão Dinâmica da Luz
19.
Colloids Surf B Biointerfaces ; 234: 113762, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38244483

RESUMO

Gastric ulcers are worrying, and their worsening conditions may result in bleeding in the internal lining of the stomach. The problem is annoying, and both patients and professionals are still not satisfied with the available treatment options. Hesperidin, a flavonoid molecule with potent anti-inflammatory and antioxidant effects, can work like witchcraft to repair gastric ulcers and preserve the stomach lining. Here, we employed a strategy that involved covering the surface of the nano-lipid carriers (NLCs) with sericin before encasing the hesperidin within (Se-He-NLC). Sericin, a biodegradable polymer increases the muco-adhesion with stomach lining and deployment of hesperidin in controlled manner. Se-He-NLCs were physico-chemically characterized for drug loading, encapsulation, particle size, morphology, drug release, chemical stability, and chemical bonding. The nanocarriers showed first order drug release in a controlled manner. Se-He-NLCs showed better in vitro permeation and ex vivo mucoadhesion, thereby by promoting the in vivo bioavailability. Se-He-NLCs also promoted the reduced glutathione (GSH) and glutathione-S-transferase (GST) levels by 2.24- and 1.61-folds, respectively in the stomach lining, and also the regulation of superoxide dismutase (SOD) and catalase (CAT) activities parallel to the control group. In addition, tissues lipid hydroperoxides (LOOH) and myeloperoxidase (MPO) activity were reduced significantly with Se-He-NLCs administration. Se-He-NLC therapy of stomach ulcers in vivo demonstrated better binding ratio and ulcer healing potential. This approach reveals huge capacity for delivering therapies to treat gastric ulcers based on the clinical significance of sericin coated hesperidin nanocarriers in gastric ulcer treatment.


Assuntos
Hesperidina , Nanopartículas , Sericinas , Úlcera Gástrica , Humanos , Ratos , Animais , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/metabolismo , Hesperidina/farmacologia , Ratos Wistar , Antioxidantes/metabolismo , Superóxido Dismutase/metabolismo
20.
Pharm Nanotechnol ; 2024 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-38284709

RESUMO

Emerging lipid-based carriers are revolutionizing drug delivery in the pharmaceutical and biomedical sciences. These innovative carriers harness the unique properties of lipids to improve the solubility, stability, and targeted delivery of therapeutic agents, ushering in a new era of precision medicine. Lipid- based carriers, such as liposomes, lipid nanoparticles, and solid lipid nanoparticles, offer several advantages. They can encapsulate both hydrophilic and hydrophobic drugs, enabling the delivery of a wide range of compounds. Additionally, lipids are biocompatible and biodegradable, minimizing the risk of toxicity. Their ability to mimic cell membranes allows for enhanced cellular uptake and controlled release, optimizing drug efficacy while minimizing side effects. Furthermore, lipid-based carriers are ideal for delivering drugs to specific sites within the body. By modifying the lipid composition, surface charge, and size, researchers can tailor these carriers to target tumours, inflamed tissues, or specific cells, improving therapeutic outcomes and reducing systemic toxicity. In summary, emerging lipid-based carriers are poised to transform pharmaceutical and biomedical sciences by addressing critical challenges in drug delivery. These carriers enhance drug stability, bioavailability, and targeted delivery, offering the potential to revolutionize the treatment of various diseases and improve patient outcomes. As research in this field continues to advance, we can expect even more sophisticated lipid-based carrier systems to emerge, further expanding the possibilities for precision medicine. This review focuses on the contribution of lipid carriers in the pharmaceutical and biomedical sciences.

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