Study on preparation and evaluation in vitro of TASS-LLCN / 中草药

ABSTRACT

Objective To prepare a new kind of preparation formulation of the total alkaloids from seed of Strychni Semen (TASS), by which could improve their drug loading content and the transdermal function. Methods TASS-LLCN were prepared by hot solvent and high pressure homogeneous method. Using encapsulation efficiency (EE) measured by ultrafiltration as index, the prescription of TASS-LLCN was optimized by response surface methodology with central composite design, and the basic properties of the optimized TASS-LLCN was evaluated. The Franz diffuser method was used to compare the transdermal capacity of both LLCN gel and ordinary gel of TASS. Results The best prescription of TASS-LLCN was as follow the content of glycerin monooleate (GMO) was 1 403.19 mg/mL, the ratio between GMO and F127 was 7.251, the drug loading content was 9.48% and the predicted encapsulation efficiency was 64.01%. The evaluation of basic properties of the optimized TASS-LLCN showed that the average grain diameter was about 186 nm, zeta potential was -33.1 mV, pH was 6.83, the stability was good. The transdermal experiment in vitro showed that the cumulate osmotic quantities in 24 h and the permeation rate of TASS-LLCN gel were both better than ordinary gel of TASS, which had obvious discrepancy (P < 0.05) and showed that LLCN could promote the absorption of active components; the skin retention volume of LLCN gel was still bigger than ordinary gel, which showed that LLCN gel of TASS could store in the skin and release the drug sustainedly. Conclusion TASS-LLCN could obviously enhance the drug loading content and the transdermal function. It is a potential new kind of preparation formulation which have the sustainable effect.