Xin Wang, Yangnan Chen, Yan Liu, Danqing Wu, Yanqiu Long, Shuangying Gui, Zhiyun Zheng, Ning He
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引用次数: 0
Abstract
The aim of this study was to improve the penetration of betulinic acid (BA) into skin efficiently by incorporating it into a nanostructured lipid carrier (NLC)-based gel. BA-NLC was prepared by the melt-emulsification and low-temperature solidification method. The optimized formulation was incorporated into the hydrogel and evaluated for pH, in vitro release, occlusion factor, and dermatokinetics. Furthermore, the transdermal penetration mechanism of the NLC gel was investigated by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), skin histological staining, and fluorescence microscopic methods. The optimized NLC showed a particle size of 153.40 nm and a high EE of 86.21%. In vitro drug release behavior of the BA-NLC gel showed higher cumulative release at 24 h (67.17 ± 2.39%) compared to the free drug (57.53 ± 2.17%). In vivo dermatokinetic studies disclosed that the BA-NLC gel presented elevated Cmax and AUC0–24 in the epidermis and dermis in contrast to the conventional gel. FT-IR and DSC research indicated that the NLC formulations changed the configuration of skin keratin and augmented lipid fluidity, thus facilitating the percutaneous permeability of actives. Fluorescence microscopy also indicated improved skin penetration of the BA-NLC gel. Hence, the optimized NLC gel could potentially be a promising drug nanocarrier to boost skin drug penetration and retention.
期刊介绍:
Biopharmaceutics & Drug Dispositionpublishes original review articles, short communications, and reports in biopharmaceutics, drug disposition, pharmacokinetics and pharmacodynamics, especially those that have a direct relation to the drug discovery/development and the therapeutic use of drugs. These includes:
- animal and human pharmacological studies that focus on therapeutic response. pharmacodynamics, and toxicity related to plasma and tissue concentrations of drugs and their metabolites,
- in vitro and in vivo drug absorption, distribution, metabolism, transport, and excretion studies that facilitate investigations related to the use of drugs in man
- studies on membrane transport and enzymes, including their regulation and the impact of pharmacogenomics on drug absorption and disposition,
- simulation and modeling in drug discovery and development
- theoretical treatises
- includes themed issues and reviews
and exclude manuscripts on
- bioavailability studies reporting only on simple PK parameters such as Cmax, tmax and t1/2 without mechanistic interpretation
- analytical methods