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1.
J Microencapsul ; 37(5): 341-354, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32293928

RESUMO

Aim: The aim of this project is to improve the therapeutic effectiveness, permeation and retention of clobetasol propionate in sebaceous glands by reporting the use of Squarticles as lipidic nanosystem.Methods: Homogenisation method is used for the formulation of Squarticles (nanoemulgel) which was characterised on the basis of size, polydispersity index (PDI), viscosity, spreadability, DSC, % in vitro release, in vitro skin permeation deposition studies, and in vivo studies, scanning electron microscopic (SEM) and physical storage stability studies were done at different temperature conditions, i.e. 4 ± 2 °C, 25 ± 2 °C and 45 ± 2 °C for a period of 6 months for drug and formulation.Result: The morphological characterisation of prepared nanoemulsion shows small spherical shape and uniform size distribution as observed in the Scanning electron microscopic (SEM), having mean size (240.5 ± 9.2) and mean size distribution (0.282 ± 0.03) and zeta potential (-51.21). The drug release from optimised nanoemulsion (F2) in PBS (pH 5.5) was approximately 84.24 ± 1.35%, nanoemulgel formulations showed the release of 66.83 ± 2.05% while marketed gel showed the release of 57.67 ± 1.63% after 24 h. The cumulative percentage retention of clobetasol propionate loaded nanoemulgel was 63 ± 1.28% which was more than the marketed formulation (23.12% ±0.54). Physical stability studies show that formulation is more stable in cold condition. Further, the stability of active ingredient in gel formulation was determined using HPLC which shows around 15 ± 0.84% of loss in its activity.Conclusion: The present work has demonstrated the use of Squarticles as a novel carrier for treatment of plaque psoriasis by enhancing the better permeation, increasing skin retention, and enhances the effect of drug. The study also shows that the formulation is more stable in cold condition.


Assuntos
Clobetasol/administração & dosagem , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Nanopartículas/química , Psoríase/tratamento farmacológico , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Modelos Animais de Doenças , Feminino , Géis , Lipídeos/química , Masculino , Microscopia Eletrônica de Varredura , Tamanho da Partícula , Ratos , Ratos Wistar , Reologia , Glândulas Sebáceas/efeitos dos fármacos , Absorção Cutânea , Temperatura
2.
Curr Mol Pharmacol ; 14(3): 399-411, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32598275

RESUMO

BACKGROUND: Psoriasis is an autoimmune disease of the skin with lapsing episodes of hyperkeratosis, irritation, and inflammation. Numerous traditional and novel drug delivery systems have been used for better penetration through psoriatic barrier cells and also for retention in the skin. As there is no effective remedy for better penetration, and retention is there because of the absence of an ideal carrier for effective and safe delivery of antipsoriatic drugs. OBJECTIVES: The main objective of this project is to develop a Squalene integrated NLC based carbopol 940 gel to create a local drug depot in the skin for improved efficacy against psoriasis. METHODS: Homogenization method is used for the formulation of Nanostructured Lipid Carrier, which was characterized on the basis of size, entrapment efficiency, polydispersity index (PDI), viscosity, spreadability, DSC, zeta potential, % in vitro release, in vitro skin permeation and retention studies, physical storage stability studies. In vivo studies can use other alternative models for induction of psoriasis by severe redness, swelling macroscopically, and microvascular dilation edema lasting for 10 days. Furthermore, histopathology study was done to asses changes in the skin. CONCLUSION: The optimized formulation of nanostructured lipid carrier-based gel has shown significant and sustained release of clobetasol propionate. Furthermore, this formulation has also shown retention in skin because of squalene as it is a sebum derived lipid, which shows an affinity towards the sebaceous gland.


Assuntos
Nanoestruturas , Psoríase , Clobetasol/uso terapêutico , Portadores de Fármacos , Humanos , Lipídeos/uso terapêutico , Psoríase/tratamento farmacológico
3.
Artif Cells Nanomed Biotechnol ; 46(sup2): 295-305, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30043651

RESUMO

Cancer nanotherapeutics are swiftly progressing and are being applied to solve several limitations of conventional drug delivery systems such as non-specific biodistribution and targeting, lack of water solubility and poor oral bioavailability. Advances in protein engineering and materials science have contributed to novel nanoscale targeting approaches that may bring new hope to cancer patients. Several therapeutic nanocarriers have been approved for clinical use. Nanoparticles have been designed for optimal size and surface characteristics to improve their biodistribution and to increase their circulation time in the bloodstream. By selectively using the unique pathophysiology of tumours, such as their enhanced permeability and retention effect nanotherapeutics are able to carry loaded active drug to cancer cells. In addition to this passive targeting mechanism, active targeting strategies using ligands or antibodies directed against selected tumour targets magnify the specificity of these therapeutic nanoparticles. Drug resistance, another obstacle can also be overcome or reduced by using nanoparticles. Multifunctional and multiplex nanoparticles are now being actively investigated and are on the horizon as the next generation of nanoparticles, facilitating personalized and tailored cancer treatment.


Assuntos
Portadores de Fármacos/química , Nanopartículas/química , Neoplasias/tratamento farmacológico , Animais , Portadores de Fármacos/metabolismo , Humanos
4.
Curr Pharm Des ; 24(33): 3934-3950, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30387390

RESUMO

BACKGROUND: Psoriasis is an autoimmune disease of the skin with lapsing episodes of hyperkeratosis, irritation and inflammation. Numerous methodologies and utilization of different antipsoriatic drugs with various activity methods and routes of administration have been investigated to treat this terrifying sickness. In any case, till date, there is no remedy for psoriasis because of the absence of an ideal carrier for effective and safe delivery of antipsoriatic drugs. OBJECTIVE: Among the different methods of medications for psoriasis, in the greater part of patients, topical treatment is most commonly utilized. For topical formulations, utilization of conventional excipients could fill the need just to a restricted degree. With the revelation of more up to date biocompatible and biodegradable materials like phospholipids, and Novel drug delivery technologies like liposomes, solid lipid nanoparticles (SLNs), microemulsions, and nanoemulsions, the possibility to enhance the efficiency and safety of the topical products has expanded to a great extent. Understanding the topical delivery aspects and that of outlining and creating different carrier systems have been enhanced that got further novelty to this approach. CONCLUSION: Present review is an attempt to contemplate on psoriasis as far as improved comprehension of the dermal delivery perspectives and at present accessible treatment alternatives, significant preventions in psoriasis treatment, late advancements in the conveyance of different antipsoriatic drugs through novel colloidal drug transporters.


Assuntos
Antipsicóticos/uso terapêutico , Nanopartículas/química , Psoríase/tratamento farmacológico , Animais , Antipsicóticos/administração & dosagem , Antipsicóticos/química , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Humanos , Estrutura Molecular , Nanopartículas/administração & dosagem
5.
J Indian Soc Periodontol ; 22(4): 317-321, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30131623

RESUMO

AIM: The aim of the present study is to compare the amount of remaining calculus, loss of tooth substance, and roughness of root surface after scaling and root planing with or without magnification loupes using scanning electron microscope. MATERIALS AND METHODS: In the study, 30 teeth indicated for extractions due to severe chronic generalized periodontitis were included in the study. In test Group I, scaling and root planing was performed without magnification loupes, and in test Group II, scaling and root planing was performed with magnification loupes before extraction. In control Group III, no procedure was performed. After scaling and root planing, teeth were extracted followed by preparation of specimens. Specimens were then sent for scanning electron microscope study. RESULTS: Statistically significant (P ≤ 0.05) differences were found among different test groups. Results showed that test Group II with magnification loupes had less remaining calculus and smoother surface with lesser amount of loss of cementum layer. CONCLUSION: From this, it was concluded that test Group II was more efficient in root debridement than test Group 1, so scaling and root planing done with magnification loupes will cause less damage to the tooth surface.

6.
Artif Cells Nanomed Biotechnol ; 45(6): 1-9, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27388946

RESUMO

The aim of the present study is to develop embelin-loaded enteric-coated microspheres and investigate their pharmacological potential in acetic acid induced ulcerative colitis. The optimized formulation of embelin-loaded microspheres has shown significant sustained release of embelin. Further this formulation significantly reduced the ulcer activity score and oxidative stress, and attenuated the inflammatory changes. Thus it may be concluded that embelin-loaded enteric-coated microspheres have shown delayed release capacity than plain embelin and exerts colon ulcer protective effect in rats.


Assuntos
Benzoquinonas , Materiais Revestidos Biocompatíveis , Colite Ulcerativa/prevenção & controle , Microesferas , Ácido Acético/toxicidade , Animais , Benzoquinonas/química , Benzoquinonas/farmacologia , Materiais Revestidos Biocompatíveis/química , Materiais Revestidos Biocompatíveis/farmacologia , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/metabolismo , Modelos Animais de Doenças , Estresse Oxidativo/efeitos dos fármacos , Ratos
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