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1.
J Biomater Sci Polym Ed ; 35(9): 1400-1420, 2024 06.
Artigo em Inglês | MEDLINE | ID: mdl-38502545

RESUMO

The aim of this study was to develop and evaluate the transdermal patch formulations of nifedipine. The patch formulations containing nifedipine were prepared and optimized with different ratios of vinyl and cellulose-derived polymers, drug contents, and permeation enhancers. Among the various formulations, the patch formulation containing a 1:5 ratio of ethyl cellulose and polyvinyl pyrrolidone was selected for ex vivo pharmacokinetic study based on in vitro permeation studies using stratum corneum of the pig's skin. The cumulative percentage release after the transdermal administration of the optimized patch formulation was 71.43%, and the plasma concentration of nifedipine was maintained for 16 hrs. The physicochemical evaluation study including flatness, thickness, moisture content and uptake, drug content in vitro release, and ex vivo permeation indicated satisfactory results. The formulation batch with clove oil as a penetration enhancer has shown better ex vivo permeation as compared to the formulations without enhancers and another synthetic enhancer. These results suggest that the optimized patch formulation Q3 could be further developed for clinical applications, providing the therapeutic plasma level of nifedipine over an extended period. Hence analyzing the results of the evaluation tests, in vitro and ex vivo data on the preparation and optimization of nifedipine-loaded transdermal patch, it can be concluded that the formulation shows its feasibility as an effective transdermal delivery system for nifedipine.


Assuntos
Administração Cutânea , Celulose , Nifedipino , Óleos Voláteis , Absorção Cutânea , Adesivo Transdérmico , Nifedipino/farmacocinética , Nifedipino/administração & dosagem , Nifedipino/química , Animais , Celulose/química , Celulose/análogos & derivados , Suínos , Absorção Cutânea/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/administração & dosagem , Óleos Voláteis/farmacocinética , Pele/metabolismo , Liberação Controlada de Fármacos , Permeabilidade , Masculino
2.
Oncol Rev ; 13(2): 417, 2019 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-31410248

RESUMO

Glioblastoma multiform (GBM) is a heterogeneous group of primary neoplasm resistant to conventional therapies. Due to their infiltrative nature it not fully isolated by aggressive surgery, radiation and chemotherapy showing poor prognosis in glioma patients. Unfortunately, diagnosed patients die within 1.5-2 year treatment schedule. Currently temozolomide (TMZ) is the first choice for the prognosis of GBM patients. TMZ metabolites methyl triazen imidazol carboxamide form complex with alkyl guanine alkyl transferase (O6 MGMT- DNA repair protein) induced DNA damage following resistance properties of TMZ and inhibit the overall survival of the patients. Last few decades different TMZ conjugated strategy is developed to overcome the resistance and enhance the chemotherapy efficacy. The main aim of this review is to introduce the new promising pharmaceutical candidates that significantly influence the therapeutic response of the TMZ in context of targeted therapy of glioblastoma patients. It is hoped that this proposed strategy are highly effective to overcome the current resistance limitations of TMZ in GBM patients and enhance the survival rate of the patients.

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