PT  - JOURNAL ARTICLE
AU  - Ebrahimnejad, P.
AU  - Dinarvand, R.
AU  - Sajadi, S. A.
AU  - Atyabi, F.
AU  - Ramezani, F.
AU  - Jaafari, M. R.
TI  - Preparation and Characterization of Poly Lactide-co-glycolide Nanoparticles of SN-38
DP  - 2009 Nov 01
TA  - PDA Journal of Pharmaceutical Science and Technology
PG  - 512--520
VI  - 63
IP  - 6
4099  - http://journal.pda.org/content/63/6/512.short
4100  - http://journal.pda.org/content/63/6/512.full
SO  - PDA J Pharm Sci Technol2009 Nov 01; 63
AB  - SN-38 (7-ethyl-10-hydroxycamptothecin) is the active metabolite of irinotecan (CPT-11), which is 100–1000-fold more cytotoxic than irinotecan. Nonetheless, the extreme hydrophobicity of SN-38 has prevented its clinical use. SN-38 is poorly soluble in aqueous solutions, and it is practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. One way of improving the solubility and stability of SN-38 is to formulate the drug into nanoparticles. Incorporation of cytotoxic agents into nanoparticles has also shown increased toxicity. In this study, poly lactide-co-glycolide was used for the preparation of nanoparticles of SN-38. The nanoparticles were fabricated by an emulsification/solvent evaporation method. The effect of several variables on nanoparticle characteristics was evaluated, including the ratio of drug–polymer, the amount of the poly vinyl alcohol as surfactant, and the internal phase volume/composition. The SN-38 encapsulation efficiency and the particle size distribution were optimized by varying these parameters. Nanoparticles were spherical with a relatively mono-dispersed size distribution. As the ratio of acetone to dichloromethane increased, a considerable decrease in the particle size of nanoparticles was achieved. The encapsulation efficiency of all samples was more than 80%. Changing the poly vinyl alcohol concentration in the external phase had some effects on size and morphology and encapsulation efficiency. It was shown that SN-38 nanoparticles are considerably stable in a long-term stability study.© PDA, Inc. 2009