Chitin microcapsules are prepared using a simple desolvation or nonsolvent addition phase separation method with 6-mercaptopurine (6-MP) as a reference core. Chitin with a molecular weight about 400,000 is used to prepare different core loaded microcapsules. The drug release rates of chitin microcapsules prepared by simple desolvation or nonsolvent addition method have different release profiles which are related to the rate of phase separation. With respect to the solubility parameter difference (delta delta) value between solvent and nonsolvent, the release rate of 6-MP from microcapsules decreases with increasing delta delta of the preparative system. The chitin beads show poor swelling properties and their release rates are pH-dependent. Sustained release of 6-MP from chitin microcapsules in low pH and neutral medium can be accomplished. To determine if the drug release from the polymer matrix is via a diffusion controlled or by an erosion controlled process, 6-MP release profiles of various chitin microcapsules degraded by lysozyme are investigated. The drug-release patterns of the chitin microcapsules prepared by nonsolvent addition (acetone, n-propanol, n-butanol) and simple desolvation in acetone are not only diffusion but also lysozyme digestion influenced. Whereas, by using water or ethanol as nonsolvent or desolvating agent, release profiles of the microcapsules prepared by nonsolvent addition and the simple desolvation method seem to be little affected by enzyme degradation. These results indicate that chitin might prove useful as a polymer carrier for the sustained release of drugs.
Chitin [poly-(N-acetyl-1,4-beta-D-glucopyranosamine)] microcapsules were prepared by the simple desolvation and the non-solvent addition phase separation methods. In the simple desolvation method, chitin droplets were dropped into the desolvation agent (water, ethanol, or acetone) and microcapsules soon formed. Several solvent-nonsolvent pairs: N,N-dimethylacetamide (DMAc)-water, DMAc-ethanol, DMAc-propanol, DMAc-n-butanol, and DMAc-acetone with different solubility parameter difference, (delta delta) were chosen to prepare chitin microcapsules containing 6-mercaptopurine by using the non-solvent-addition phase separation method. The results showed that the surface morphology and release behaviour of the microcapsules were greatly affected by different solvent-nonsolvent pairs. The surface of microcapsules prepared from the system of high delta delta was more smooth than those from the systems of low delta delta. The drug content using the simple desolvation method increased with decreasing delta delta because of the higher film formation rate of the microcapsules. On the other hand, the drug content using the nonsolvent addition method was lower than that using the simple desolvation method because of the dispersion forces, applied by mechanical stirring. Microcapsules prepared by the simple desolvation method had a narrower size distribution and larger mean size than those prepared by the nonsolvent addition method.
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