Optimization and evaluation of pluronic lecithin organogels as a transdermal delivery vehicle for sinomenine

Abstract

The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box-Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (Jss) of SIN from PLO was 146.55 ± 2.93 μg/cm(2)/h, significantly higher than that of gel (120.39 μg/cm(2)/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 μg/cm(2), significantly larger than that from gel (6.01 ± 0.04 μg/cm(2)). In vivo skin microdialysis studies showed that the maximum concentration (Cmax) of SIN from PLO in "permeation study" and "drug-deposition study" were 150.27 ± 20.85 μg/ml and 67.95 μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.

Formulation and evaluation of novel controlled release of topical pluronic lecithin organogel of mefenamic acid

“…Thus, the percent cumulative amount of drug release was reduced, as the viscosity of the formulations increased and these results were in accordance with earlier study findings (Pandey et al, 2010). The gelation temperature range of our formulations lies below normal body temperature because our formulation exists in gel state and similar findings were also reported by Ba et al (2016). The skin irritation study was also performed on rats and all formulations showed no detectable sign of skin irritation, indicating excellent compatibility with skin.…”

Sinomenine hydrochloride-loaded dissolving microneedles enhanced its absorption in rabbits

“…These tests demonstrated that SH-DM has enough mechanical strength to create pores for drug penetrating into skin. [52][53][54] . Cumulative permeation quantity of SH from SH-G and SH-DM was determined via the in vitro permeation study (Figure 3).…”

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“…The sample was analyzed to determine the drug content by HPLC at 254 nm. The release kinetics of the formulations were calculated, and release patterns for those formulation were analyzed using three mathematical models: -(a) zero order kineticsreleased amount per unit area (mg/cm 2 ) against the time (h), (b) Higuchi kineticsreleased amount per unit area (mg/cm 2 ) against the square root of time (h) and (c) first order kineticslog of released amount per unit area (mg/cm 2 ) against the time (h) 9,47 .…”