Shakshuki Ayah, Agu Remigius U
Biopharmaceutics and Drug Delivery Lab, Halifax, NS, Canada.
Int J Pharm Compd. 2019 Nov-Dec;23(6):496-503.
The objective of this study was to investigate the effect of Lipoderm Cream, VersaBase Gel, and Emollient Cream on the release and permeation of gabapentin formulated for neuropathic pain. Gabapentin of different strengths (1%, 5%, and 10%) was compounded with the bases, diffusion of the drug from thebases, and permeation through artificial skin model studied with Franz diffusionsystem. Steady-state flux, cumulative permeation, and lag times were calculated,and release mechanisms modelled with first order, second-order, Higuchi, Korsmeyer-Peppas, and Hixon-Crowell kinetic models. Gabapentin recovery from VersaBase Gel, Lipoderm Cream, and Emollient Cream was 100.8 ± 2.7%, 101.3 ± 1.2%, and 104.9 ± 3.3%, respectively. Gabapentin completely diffused out of the three bases within 6 hours of application according to the Higuchi model. Flux of the drug appeared to be concentration-dependent with no permeation occurring at 1% strength. Whereas, 5% and 10% strengths in Lipoderm Cream permeated the skin rapidly, the same concentrations in Emollient Cream and VersaBase Gel required 60-minutes and 120-minutes lag times, respectively. For the three bases, a strong correlation was observed between lag times and flux. The overall permeation in VersaBase Gel and Lipoderm Base was not significantly different (P>0.05). However, Emollient Cream resulted in a significantly lower total permeation compared to other bases (P<0.05). As the formulations are for pain management, products with no lag times and higher flux are preferable. Although VersaBase Gel and Emollient Cream displayed some gabapentin permeability, it is important to consider gabapentin stability in these bases prior to use.
本研究的目的是调查脂质体乳膏、VersaBase凝胶和润肤霜对用于神经性疼痛的加巴喷丁释放和渗透的影响。将不同浓度（1%、5%和10%）的加巴喷丁与基质混合，利用Franz扩散池研究药物从基质中的扩散以及透过人工皮肤模型的渗透情况。计算稳态通量、累积渗透量和滞后时间，并用一级、二级、Higuchi、Korsmeyer-Peppas和Hixon-Crowell动力学模型对释放机制进行建模。加巴喷丁从VersaBase凝胶、脂质体乳膏和润肤霜中的回收率分别为100.8±2.7%、101.3±1.2%和104.9±3.3%。根据Higuchi模型，加巴喷丁在应用后6小时内完全从三种基质中扩散出来。药物通量似乎与浓度有关，1%浓度时无渗透发生。然而，脂质体乳膏中5%和10%的浓度能快速渗透皮肤，润肤霜和VersaBase凝胶中相同浓度分别需要60分钟和120分钟的滞后时间。对于这三种基质，滞后时间和通量之间存在强相关性。VersaBase凝胶和脂质体基质中的总体渗透无显著差异（P>0.05）。然而，与其他基质相比，润肤霜导致的总渗透显著更低（P<0.05）。由于这些制剂用于疼痛管理，无滞后时间且通量更高的产品更可取。尽管VersaBase凝胶和润肤霜显示出一定的加巴喷丁渗透性，但在使用前考虑加巴喷丁在这些基质中的稳定性很重要。
