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Controlled Release of 9-nitro-20(S)-camptothecin From Methoxy Poly(ethylene glycol)-poly(D,L-lactide) Micelles

Controlled Release of 9-nitro-20(S)-camptothecin From Methoxy Poly(ethylene glycol)-poly(D,L-lactide) Micelles

J M Gao, J Ming, B He, Z W Gu, X D Zhang

Biomed Mater. 2008 Mar;3(1):015013.

PMID: 18458500

Abstract:

9-nitro-20(S)-camptothecin (9-NC) is a potent topoisomerase-I inhibitor, and it was applied for clinical trials in cancer treatment. However, the applications of 9-NC were limited by its poor solubility and instability. In order to overcome these disadvantages, 9-NC was encapsulated in amphiphilic copolymer micelles composed of methoxy poly(ethylene glycol)-b-poly(D,L-lactide) (mPEG-PDLLA, PELA). Three diblock copolymers with different PDLLA chain lengths were synthesized. The critical micelle concentration was varied from 10(-4) g L(-1) to 10(-2) g L(-1). The 9-NC loaded micelles were nanospheres with diameters ranging from 30 nm to 60 nm. The relationship between the composition of copolymers and the drug loading content was discussed. The encapsulation of micelles improved the solubility of 9-NC greatly. The solubility of 9-NC in micelle M1 was about 250 times higher than that of 9-NC in a phosphate buffer solution (PBS). The stability of 9-NC in micelles was also promoted. After being incubated in PBS for 160 min, 80% of 9-NC in micelles existed as an active lactone form, while 85% of 9-NC in PBS were transferred to an inactive carboxylate salt form. The release experiments were carried out in PBS and the results showed that the release processes were controllable.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS74325	Methoxy poly(ethylene glycol)-b-poly(D,L-lactide)			Price

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