Department of Pharmaceutical Technology, Naresuan University, Phitsanulok, Thailand.
Int J Cosmet Sci. 2005 Apr;27(2):89-99. doi: 10.1111/j.1467-2494.2004.00250.x.
Synopsis The aim of this study was to develop hydrogel patch using crosslinked chitosan-starch as polymeric matrix for controlling the release of the natural alpha-hydroxy acid (AHA) contained in the extract of tamarind's fruit pulp. The chitosan (MW 100 000) was blended with corn, tapioca or rice starch in various ratios and then crosslinked with glutaraldehyde. The physical characteristics, mechanical resistance, bio-adhesion property and surface morphology of the prepared hydrogel patches with and without the extract were investigated. The release patterns of the hydrogel patches containing the extract were investigated by measuring the amount of tartaric acid, a major AHA present in the tamarind's fruit pulp extract, accumulated in the receptor medium of the vertical diffusion cell at various time intervals over a period of 6 h. The results indicated that the formulations of chitosan : corn starch 4.5 : 0.5 with glutaraldehyde 0.02% w/w (C(4.5)C(0.5)G(0.02)) or 0.04% w/w (C(4.5)C(0.5)G(0.04)), chitosan : tapioca starch 4.5 : 0.5 with glutaraldehyde 0.04% w/w (C(4.5)T(0.5)G(0.04)) or 0.05% w/w (C(4.5)T(0.5)G(0.05)), and chitosan : rice starch 4.5 : 0.5 with glutaraldehyde 0.04% w/w (C(4.5)R(0.5)G(0.04)) and chitosan : rice starch 4.0 : 1.0 with glutaraldehyde 0.03% w/w (C(4.0)R(1.0)G(0.03)) provided the flexible and elastic patches with good bio-adhesive property. The tensile strength values ranged from 5 to15 N mm(-2) and the elasticity ranged from 30 to 60%. The addition of the extract in these formulations significantly increased the tensile strength values of the obtained patches. The patch of C(4.0)R(1.0)G(0.03) formulation containing the extract showed relatively highest porosity, corresponding to its highest amount (12.02 +/- 0.33 mg) and rate (0.452 +/- 0.012 mg mm(-2) min(-1/2)) of tartaric acid released. The amounts of tartaric acid released from the developed hydrogel patches were proportional to a square root of time (Higuchi's model), particularly the release from C(4.0)R(1.0)G(0.03) (R(2), 0.9978 +/- 0.0020) and C(4.5)R(0.5)G(0.04) (R(2), 0.9961 +/- 0.0024) patches.
概要 本研究旨在开发一种水凝胶贴片,使用交联壳聚糖-淀粉作为聚合物基质来控制天然 α-羟基酸(AHA)的释放,该 AHA 存在于罗望子果肉提取物中。壳聚糖(MW 100000)与玉米、木薯或大米淀粉以不同的比例混合,然后用戊二醛交联。研究了含有和不含有提取物的制备水凝胶贴片的物理特性、机械强度、生物粘附性和表面形态。通过测量在垂直扩散池的受体介质中在 6 小时的不同时间间隔内积累的酒石酸(罗望子果肉提取物中主要的 AHA)的量,研究了含有提取物的水凝胶贴片的释放模式。结果表明,壳聚糖:玉米淀粉 4.5:0.5 与戊二醛 0.02%(w/w)(C(4.5)C(0.5)G(0.02))或 0.04%(w/w)(C(4.5)C(0.5)G(0.04))、壳聚糖:木薯淀粉 4.5:0.5 与戊二醛 0.04%(w/w)(C(4.5)T(0.5)G(0.04))或 0.05%(w/w)(C(4.5)T(0.5)G(0.05))、壳聚糖:大米淀粉 4.5:0.5 与戊二醛 0.04%(w/w)(C(4.5)R(0.5)G(0.04))和壳聚糖:大米淀粉 4.0:1.0 与戊二醛 0.03%(w/w)(C(4.0)R(1.0)G(0.03))的配方提供了具有良好生物粘附性的柔韧且有弹性的贴片。拉伸强度值范围为 5 至 15 N mm(-2),弹性范围为 30 至 60%。在这些配方中加入提取物显著增加了所得到的贴片的拉伸强度值。含有提取物的 C(4.0)R(1.0)G(0.03)配方的贴片显示出相对较高的孔隙率,相应地其具有最高的量(12.02 +/- 0.33 mg)和释放速率(0.452 +/- 0.012 mg mm(-2) min(-1/2))的酒石酸。从开发的水凝胶贴片释放的酒石酸的量与时间的平方根成正比(Higuchi 模型),特别是从 C(4.0)R(1.0)G(0.03)(R(2),0.9978 +/- 0.0020)和 C(4.5)R(0.5)G(0.04)(R(2),0.9961 +/- 0.0024)贴片释放。