The poly(ethylene glycol)-poly(DL-lactide) block copolymers with different of molecular weight(Mw) values were synthesized to prepare the paclitaxel polymeric micelles. A flow-through cell method based on dialysis adapter for in vitro release testing of paclitaxel polymeric micelles was established, and the influences of type and molecular weight cut-off(MWCO) of dialysis membrane, flow rate of flow through cell, amount of glass beads placed in cell and sample concentration on in vitro release behavior of paclitaxel from the prepared micelles were investigated. Moreover, this method was adopted to testing the release of paclitaxel-loaded preparations, namely the self-made micelles and the commercial injection and liposomes. The results showed that the type and MWCO of the dialysis membrane had a certain effect on the in vitro release of the micelles; both flow rate and amount of glass beads had little effect on the release results; but the sample concentration had a significant effect on the test results. The release behaviors of different dosage forms of paclitaxel tested by this method were quite different, while there were only slight differences among the micelles with different MW polymers in the early stage of release.
Key words
in vitro release /
dialysis adapter /
paclitaxel /
polymeric micelle /
flow-through cell method
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References
[1] KOSTARELOS K．Rational design and engineering of delivery systems for therapeutics: biomedical exercises in colloid and surface science [J]．Adv Colloid Interface Sci,2003, 106: 147-168．
[2] SHAH V, SIEWERT M, DRESSMAN J, et al．Dissolution/in vitro release testing of special dosage forms [J]．Dissolut
Technol, 2002, 9: 6-11．
[3] SIEWERT M, DRESSMAN J, BROWN C, et al．FIP/AAPS guidelines for dissolution/in vitro release testing of novel/special dosage forms [J]．Dissolut Technol, 2003, 10:6-15．
[4] SAKORE S, CHAKRABORTY B．In vitro-in vivo correlation (IVIVC): A strategic tool in drug development[J]．J Bioequiv Bioavailab, 2011, S3: 1-12．
[5] SHEN J, BURGESS D J．In vitro dissolution testing strategies for nanoparticulate drug delivery systems: Recent
developments and challenges [J]．Drug Deliv Transl Res,2013, 3(5): 409-415．
[6] RUOZI B, TOSI G, FORNI F, et al．Ketorolac tromethamine liposomes: encapsulation and release studies [J]．J Liposome Res, 2005, 15(3-4): 175-185．
[7] XIAO C, QI X, MAITANI Y, et al．Sustained release of cisplatin from multivesicular liposomes: potentiation of
antitumor efficacy against S180 murine carcinoma [J]．J Pharm Sci, 2004, 93(7): 1718-1724．
[8] ZOLNIK B S, RATON J L, BURGESS D J．Application of USP apparatus 4 and in situ fiber optic analysis to microsphere release testing [J]．Dissolut Technol, 2005, 12:11-14．
[9] QI F, WU J, LI H, et al．Recent research and development of PLGA/PLA microspheres/nanoparticles: A review in
scientific and industrial aspects [J]．Front Chem Sci Eng,2019, 13: 14-27．
[10] PI?KIN, KAITIAN X, DENKBA? E B, et al．Novel PDLLA/PEG copolymer micelles as drug carriers [J]．J Biomater Sci Polym Ed, 1995, 7(4): 359-373．
[11] GAUCHER G, DUFRESNE M H, SANT V P, et al．Block copolymer micelles: preparation, characterization and application in drug delivery [J]．J Control Release, 109(1-3): 169-188．
[12] CHO Y W, LEE J, LEE S C, et al．Hydrotropic agents for study of in vitro paclitaxel release from polymeric micelles
[J]．J Control Release, 2004, 97(2): 249-257．
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