Bhattarai Narayan, Ramay Hassna R, Chou Shinn-Huey, Zhang Miqin
Department of Material Science and Engineering, University of Washington, Seattle,WA 98195, USA.
Int J Nanomedicine. 2006;1(2):181-7. doi: 10.2147/nano.2006.1.2.181.
Nanoparticles of approximately 10nm in diameter made with chitosan or lactic acid-grafted chitosan were developed for high drug loading and prolonged drug release. A drug encapsulation efficiency of 92% and a release rate of 28% from chitosan nanoparticles over a 4-week period were demonstrated with bovine serum protein. To further increase drug encapsulation, prolong drug release, and increase chitosan solubility in solution of neutral pH, chitosan was modified with lactic acid by grafting D,L-lactic acid onto amino groups in chitosan without using a catalyst. The lactic acid-grafted chitosan nanoparticles demonstrated a drug encapsulation efficiency of 96% and a protein release rate of 15% over 4 weeks. With increased protein concentration, the drug encapsulation efficiency decreased and drug release rate increased. Unlike chitosan, which is generally soluble only in acid solution, the chitosan modified with lactic acid can be prepared from solutions of neutral pH, offering an additional advantage of allowing proteins or drugs to be uniformly incorporated in the matrix structure with minimal or no denaturization.
用壳聚糖或乳酸接枝壳聚糖制备了直径约为10nm的纳米颗粒，用于高载药量和延长药物释放。用牛血清蛋白证明壳聚糖纳米颗粒的药物包封率为92%，在4周内的释放率为28%。为了进一步提高药物包封率、延长药物释放并增加壳聚糖在中性pH溶液中的溶解度，在不使用催化剂的情况下，通过将D，L-乳酸接枝到壳聚糖的氨基上，用乳酸对壳聚糖进行改性。乳酸接枝壳聚糖纳米颗粒在4周内的药物包封率为96%，蛋白质释放率为15%。随着蛋白质浓度的增加，药物包封率降低，药物释放率增加。与通常仅在酸性溶液中可溶的壳聚糖不同，用乳酸改性的壳聚糖可以从中性pH溶液中制备，这提供了另一个优点，即允许蛋白质或药物以最小程度的变性或不变性均匀地掺入基质结构中。
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