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1.
Pharmaceutics ; 13(9)2021 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-34575533

RESUMO

The study aims to investigate the propylene glycol-based liposomes named 'proposomes' in enhancing skin permeation of drugs with different physicochemical properties. Ibuprofen, tofacitinib citrate, rhodamine B, and lidocaine were loaded into proposomes. These drug formulations were analyzed for particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro skin permeation. The confocal laser scanning microscopy was performed on skin treated with calcein and rhodamine B laden proposomes. The transdermal delivery relative to physicochemical properties of drugs such as logP, melting point, molecular weight, solubility, etc., were analyzed. We tested the safety of the proposomes using reconstructed human skin tissue equivalents, which were fabricated in-house. We also used human cadaver skin samples as a control. The proposomes had an average diameter of 128 to 148 nm. The drug's entrapment efficiencies were in the range of 42.9-52.7%, translating into the significant enhancement of drug permeation through the skin. The enhancement ratio was 1.4 to 4.0, and linearly correlated to logP, molecular weight, and melting point. Confocal imaging also showed higher skin permeation of calcein and rhodamine B in proposome than in solution. The proposome was found safe for skin application. The enhancement of skin delivery of drugs through proposomes was dependent on the lipophilicity of the drug. The entrapment efficiency was positively correlated with logP of the drug, which led to high drug absorption.

2.
Int J Pharm ; 585: 119558, 2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32565283

RESUMO

Tofacitinib citrate (TC) has recently gained interest in treating skin disorders such as psoriasis, atopic dermatitis and baldness. Unfortunately, the oral administration shows side effects, such as decreased neutrophil counts. To this end, the topical delivery of TC can be used to reduce the risk associated with systemic exposure. However, TC shows minimal absorption via skin. Hence, the objective of this study is to enhance the skin delivery of TC using a non-invasive approach. The liposomes based on propylene glycol, named as proposomes, carrying TC, were studied. The vesicle characteristics and in vitro skin permeation were assessed. The proposomes enhanced the skin permeability of TC by 4-11 folds. The composition of proposomes was found to affect the skin permeation and deposition of TC. The proposomes were stable for at least 6 months. Overall, proposomes were effective for targeted topical drug delivery.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Lipossomos/química , Piperidinas/farmacocinética , Inibidores de Proteínas Quinases/farmacocinética , Pirimidinas/farmacocinética , Absorção Cutânea/fisiologia , Administração Cutânea , Cadáver , Química Farmacêutica/métodos , Estabilidade de Medicamentos , Humanos , Masculino , Pessoa de Meia-Idade , Tamanho da Partícula , Piperidinas/administração & dosagem , Propilenoglicol/química , Inibidores de Proteínas Quinases/administração & dosagem , Pirimidinas/administração & dosagem
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