ABSTRACT
Objective To prepare a novel drug delivery system camptothecin loaded nanogel (CPT-PPO gel),and inves-tigate its contents,physical and chemical properties and in vitro transdermal permeability.Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems (CPT-PLGA-PAMAM,CPT-PP),in which the Poly lac-tic-co-glycolic acid (PLGA ) was used to load camptothecin as the nucleus and the polyamidoamine (PAMAM ) G3.0 was wrapped in the surface of PLGA as the shell.Then the oleic acid (OA) was connected to CPT-PP to obtain the surface modified drug delivery system (CPT-PLGA-PAMAM OA,CPT-PPO).HPLC was used to determine the content of camptothecin in nanoparticles,transmission electron microscopy was applied to identify the nanoparticles morphology,and laser analyzer was used to determine the particle size.The hydroxypropyl methylcellulose (HPMC) was added as the base for the preparation of the nanogel (CPT-PPO gel) at last.The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃,the average particle size was (246.7 ± 5.4) nm and the encapsulation efficiency was up to (78.7 ± 6.9)%.Comparing to the normal gel,(CPT gel),the cumulative penetration amount and the re-tention amount in the skin of the nanogels (CPT-PPO gel,CPT-PP gel) were significant higher (P＜0.01),the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel (P＜0.05).Conclusion After modified by OA,CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.
ABSTRACT
Objective: To compare the differences in transdermal permeability, pharmacodynamics, and skin irritation of Guanjie Zhitong Patches based on two different formulations taking hot-melt pressure sensitive adhesive and rubber as matrixes. Methods: In vitro transdermal permeation was performed by means of Franz diffusion cells; The analgesic effect was evaluated by HAc-induced writhing response in mice and hot-plate test, while the anti-inflammatory action was assessed by xylem-induced ear edema in mice and albumin-induced paw edema in rats. The skin irritation of the two matrixes was investigated using guinea pig as model animal. Results: Patches based on hot-melt pressure sensitive adhesives showed better transdermal permeability, analgesic, and anti-inflammatory effects but less skin irritation than the rubber type patches. Conclusion: Hot-melt pressure sensitive adhesive is a kind of appropriate material to compose the patch matrix for Chinese herbal medicine, which has the good transdermal permeability and efficacy and less skin irritation.
ABSTRACT
Objective To investigate the in-vitro transdermal permeability of cyclovirobuxine D ethosomes.Methods Ethosomes,liposomes,saturated aqueous solution and 35.5% saturated alcohol solution of cyclovirobuxine D were prepared.The in-vitro transdermal permeability of different kinds of preparations of cyclovirobuxine D was studied by in-vitro permeation experiments.Results Cyclovirobuxine D ethosomes enhanced transdermal flux rate of cyclovirobuxine D and the enhancement ratio was 8.85,superior to liposomes and saturate alcohol.The dermatic hold-up amount of cyclovirobuxine D in 35.5% saturated alcohol solution,liposomes and ethosomes was in a decreasing sequence.Conclusion Compared with the liposomes,the ethosomes can enhance the transdermal flux rate of cyclovirobuxine D,which could increase the systematic action of the drug.