ABSTRACT
The purpose of this study was to investigate the effect of isopropyl myristate (IPM), a penetration enhancer, on the viscoelasticity and drug release of a drug-in-adhesive transdermal patch containing blonanserin. The patches were prepared with DURO-TAK87-2287 as a pressure-sensitive adhesive (PSA) containing 5% (/) of blonanserin and different concentrations of IPM. Anrelease experiment was performed and the adhesive performance of the drug-in-adhesive patches with different concentrations of IPM was evaluated by a rolling ball tack test and a shear-adhesion test. The glass transition temperature () and rheological parameters of the drug-in-adhesive layers were determined to study the effect of IPM on the mechanical properties of the PSA. The results of therelease experiment showed that the release rate of blonanserin increased with an increasing concentration of IPM. The rolling ball tack test and shear-adhesion test showed decreasing values with increasing IPM concentration. The results were interpreted on the basis of the IPM-induced plasticization of the PSA, as evidenced by a depression of the glass transition temperature and a decrease in the elastic modulus. In conclusion, IPM acted as a plasticizer on DURO-TAK87-2287, and it increased the release of blonanserin and affected the adhesive properties of the PSA.
ABSTRACT
Objective: To evaluate the in vitro percutaneous absorption profiles of ginsenoside Rh1 using ionic liquids [BMIM][Cl] as a novel permeation enhancer and to investigate the mechanism. Methods: Mice skin and porcine skin were used as skin model. Oil acid, isopropyl myristate, and menthol were used as comparing skin enhancers. The solubility of Rh1 (with or without enhancer) in water was measured by shake-flask method. Skin permeation experiment was performed using Franz diffusion cells. Skin structure change after treatment of [BMIM][Cl] was measured by FTIR. Results: By comparing with commonly used enhancers, 5% [BMIM][Cl] significantly increased the solubility of Rh1 and gave an excellent improvement on the skin penetrability of Rh1. The FTIR results suggested that [BMIM][Cl] accelerated the drug skin permeation by disrupting the lipid bilayer of skin stratum corneum. Conclusion: [BMIM][Cl] can serve as a novel skin permeation enhancer, and show a broad application prospect in transdermal drug delivery system.
ABSTRACT
Aim To investigate the influence of skin layers ( st ratum corneum and viable layer) on the percutaneous absorption of drug with or w ithout isopropyl myristate (IPM). Methods We chose theophylline (TP ) as a model drug. Patches containing saturated concentration of TP were prepare d. The in vitrotransdermal permeation experiment via different rat skin lay ers was carried out. Results The Kp of TP via stripped skin was 2.1 times larger than that via intact skin. The permea bility was en hanced when coexisted with IPM either via intact skin or via stripped skin. Conclusion IPM can significantly enhance the percutaneous absorption of TP via different skin layers. And these data and methods represent a novel appr oach to evaluate the effects of skin damage and skin disease on drug percutaneou s absorption.
ABSTRACT
OBJECTIVE:To investigate the influence of skin layers(stratum corneum and dermis)on the percutaneous absorption of drug.METHODS:We chose hydroquinone(HQ)as a model drug and carried out in vitro permeation experiment with Franz device.The in vitro transdermal permeation was compared between HQ plus isopropyl myristate(IPM)and HQ alone.RESULTS:The permeability coefficient(Kp)of HQ via split skin was 3.29 times larger than that via whole skin layer.The permeability was enhanced 4.95 times(whole skin layer)and 7.49 times(skin without stratum corneum)respectively when coexisting with IPM via intact or via split skin.CONCLUSION:These data and methods represent a novel approach to evaluate the effects of skin damage and skin disease on drug percutaneous absorption.