Sinomenine-loaded microcapsules fabricated by phase reversion emulsification-drying in liquid method: An evaluation of process parameters, characterization, and released properties

Abstract

Sinomenine is a natural alkaloid with important biological activities (e.g. anti-cancer, antiinflammatory, and anti-allergic). However, the unstability and short half-life absolutely limited its application to foods. Microencapsulation technology can offer a way to solve these issues. In this study, polylactic acid microcapsules loading sinomenine hydrochloride were fabricated by phase inversion emulsification-drying in liquid technique. The results showed that microcapsules had nice spherical shape, uniform particle size, and free flowing. The encapsulation efficiency was 89.2% and drug loading was 8.9% under the optimal conditions. In vitro release assays demonstrated that release of sinomenine from microcapsules was sustained and slow. Moreover, it was found that the sinomenine release fitted Fickian diffusion mechanism. The results of cytotoxicity study showed that sinomenine-loaded microcapsules were biocompatible. Sinomenine-loaded

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review

“…In the same year, W. Zhang et al reported the benefits of SH polylactic acid microcapsules, which inhibited both bacteria and MDA-MB-231 cells. It (15.2 mM) exhibited a sustained release effect, a slower release rate, good biocompatibility, and no apparent cytotoxicity to normal L929 cells [ 46 ]. Concurrently, D. Zhang et al announced the radiosensitive effect of SH on cervical cancer cells.…”

Co-amorphous Systems of Sinomenine with Platensimycin or Sulfasalazine: Physical Stability and Excipient-Adjusted Release Behavior

“…Then, the mold was compressed under 160 MPa for 5 min using a hydropress to obtain the tablets for in vitro release experiments. The release tests were performed in small cups containing 100 mL of pH 6.8 PBS with a rotation speed of 50 rpm using small paddles at 37 ± 0.5 °C for 6 h. At preset intervals (5,10,20,30,60,120,240, and 360 min), 1 mL of solution in each cup was extracted and replaced by equivoluminal fresh PBS. The acquired samples were filtered using polycarbonate filters (0.22 μm) and analyzed by UPLC.…”

“…Multi-dose therapy with SIN-HCl leads to violent fluctuation of blood drug concentration, which may result in serious side effects. Although some sustained release strategies of SIN-HCl have been developed, the marketed SIN-HCl tablets still required administration twice per day, suggesting that novel and long sustained release strategies for SIN are needed. − …”