Chen Y, Burton M A, Codde J P, Napoli S, Martins I J, Gray B N
Department of Surgery, University of Western Australia, Royal Perth Hospital.
J Pharm Pharmacol. 1992 Mar;44(3):211-5. doi: 10.1111/j.2042-7158.1992.tb03583.x.
A comparison study of doxorubicin loading, release characteristics and stability within sodium and hydrogen forms of ion-exchange resin microspheres has been performed. It was demonstrated that resins in the Na+ form, although having lower drug loading capacity, showed similar release profiles to resins in the H+ form but still maintain all the drug activity. Resins in the H+ form, despite having high drug loading capacity, caused drug degradation within microspheres due to their strong acidic nature. Therefore, in comparison with the H+ form, resins in the Na+ form can be considered as better carriers for doxorubicin in terms of sustaining the release of drug and maintaining drug activity. Other factors such as the degree of resin cross-linkage and drug/resin mixing time have also been examined in relation to drug loading and release characteristics. Overall, this study demonstrated the significance of the characteristics of matrix materials and their influence on the drug activity and microsphere performance in-vitro.
对阿霉素在离子交换树脂微球的钠型和氢型中的负载、释放特性及稳定性进行了比较研究。结果表明，Na⁺型树脂虽然载药量较低，但释放曲线与H⁺型树脂相似，且仍保留所有药物活性。H⁺型树脂尽管载药量高，但因其强酸性导致微球内药物降解。因此，与H⁺型相比，就维持药物释放和保持药物活性而言，Na⁺型树脂可被视为阿霉素更好的载体。还研究了树脂交联度和药物/树脂混合时间等其他因素与药物负载和释放特性的关系。总体而言，本研究证明了基质材料特性及其对体外药物活性和微球性能影响的重要性。
