Optimization of elastic transfersomes formulations for transdermal delivery of pentoxifylline

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• 作者：Ahmed H. AL Shuwaili^a ; Bazigha K. Abdul Rasool^b ; ^{bazigha@dpc.edu" class="auth_mail" title="E-mail the corresponding author} ; ^{bazigha_rasool@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; ; Alaa A. Abdulrasool^c
• 关键词：Pentoxifylline (PubChem CID ; 4740) ; Sodium cholate (PubChem CID ; 23668194) ; Phosphatidylcholine (PubChem CID ; 45266626) ; Tween 20 (PubChem CID ; 486150) ; Tween 80 (PubChem CID ; 9920342) ; Span 20 (PubChem CID ; 16218599)
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2016
• 出版时间：May 2016
• 年：2016
• 卷：102
• 期：Complete
• 页码：101-114
• 全文大小：2699 K

文摘

Pentoxifylline (PTX) is a xanthine derivative indicated in treatment of intermittent claudication and chronic occlusive arterial diseases. It has low oral bioavailability and short half-life; thus, it was considered as a good candidate drug for the transdermal transfersomes formulation. In the present study, an attempt has been made for development, in-vitro and in-vivo evaluation of transdermal transfersomes using sodium cholate (SC) and non-ionic surfactants as edge activators. The optimal formulation, F4_(Gcholate), exhibited drug entrapment efficiency of 74.9 ± 1.6%, vesicles elasticity of 145 ± 0.6 (mg s⁻¹ cm⁻²), zeta potential of −34.9 ± 2.2 mV, average vesicle diameter of 0.69 ± 0.049 μm with PDI of 0.11 ± 0.037 and permeation flux of 56.28 ± 0.19 μg cm⁻² h⁻¹. It attained a prolonged drug release where 79.1 ± 2.1% of PTX released after 10 h of the run. The drug release kinetic obeys Higuchi model (R² = 0.997) with Fickian diffusion mechanism. Moreover, the formula enhanced drug permeation through the excised rat’s skin predominantly via the carrier-mediated mechanism by 9.1 folds in comparison with the control. Results of the in vivo pharmacokinetics study in male volunteers showed that F4_(Gcholate) transfersomes formulation increased PTX absorption and prolonged its half-life comparing to the commercial oral SR tablets. Hence, the elastic transfersomes formulation of PTX possesses admirable potential to avoid drug metabolism, improve PTX bioavailability and sustain its release.