The controlled release of a drug from biodegradable chitosan gel beads.
The controlled release of a drug from biodegradable chitosan gel beads.
复制标题
从可生物降解的壳聚糖凝胶珠中控制药物的释放。
DOI：
10.1248/cpb.48.579
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发表时间：
2000
影响因子：
1.7
通讯作者：
S. Kawashima
中科院分区：
文献类型：
--
作者：
K. Kofuji;T. Ito;Y. Murata;S. Kawashima
壳聚糖（CS）在pH高于12的溶液中形成凝胶，并且在10%氨基酸溶液中在pH约9时发生凝胶化。在本文中，我们研究了这种新的CS凝胶珠的酶降解和药物释放曲线。CS凝胶珠的降解性受CS性质的影响，例如脱乙酰度。与仅用NaOH制备的凝胶相比，作为模型药物的泼尼松龙（PS）从CS凝胶珠中的释放持续显著。然而，释放不能通过用于制备CS凝胶珠的溶液中NaOH浓度的增加来维持。我们还研究了通过应用硫酸软骨素（Cho）和CS之间形成的复合物来控制药物从CS凝胶珠中的释放。经Cho处理的CS凝胶珠中PS的释放时间延长，且释放模式不受处理时间的影响。用PS粉末达到50%药物释放的时间约为5分钟，在含有10%甘氨酸（Gly）（pH 9.0）的CS凝胶珠中约为200分钟，在用Cho处理的含有10%Gly（pH 9.0）的CS凝胶珠中约为330分钟。因此，CS凝胶珠作为持续药物递送的载体是有希望的，并且CS凝胶珠的降解可以通过CS的脱乙酰化程度来控制。
Chitosan (CS) forms a gel in solutions with a pH above 12, and the gelation occurs at pH of about 9 in 10% amino acid solutions. In this paper, we investigated the enzymatic degradation and the drug release profile of this novel CS gel beads. The degradability of the CS gel beads was affected by the CS properties, e.g. the degree of deacetylation. The release of prednisolone (PS), as a model drug, from the CS gel beads was sustained significantly compared with the gel prepared with NaOH only. However, the release was not able to be sustained by the increment of NaOH concentration in the solution employed for the preparation of CS gel beads. We also investigated the control of drug release from CS gel beads by application of a complex formed between chondroitin sulfate (Cho) and CS. The release of PS from the CS gel beads treated with Cho was prolonged, and the release pattern was not affected by the treatment time. The time to 50% drug release was about 5 min with PS powder, about 200 min in CS gel beads with 10% glycine (Gly) (pH 9.0), and about 330 min in the CS gel beads with 10% Gly (pH 9.0) treated with Cho. Thus CS gel beads appear promising as a vehicle for sustained drug delivery, and the degradation of CS gel beads may be controlled by the degree of deacetylation of CS.