Paclitaxel-loaded poly(L-lactic acid) microspheres 3: blending low and high molecular weight polymers to control morphology and drug release

International Journal of Pharmaceutics
Richard T Liggins, Helen M Burt

Abstract

Microspheres were prepared from paclitaxel and binary polymer blends incorporating 1, 3, 40k and 100k g/mol PLLA. Thermal analysis was performed by DSC and in vitro paclitaxel release profiles were determined at 37 degrees C in phosphate buffer using an HPLC assay. In microspheres made with 3k/40k PLLA blends, the glass transition (Tg), crystallinity and melting temperature (Tm) all decreased with an increasing proportion of low molecular weight polymer in the blend. Similar trends were observed for 1k/100k blends. Tm values ranged from 175 to 110 degrees C and Tg values between 66 and 37 degrees C. However, for 1k/100k blends, melting point depression was linearly dependent on blend composition when plotted as 1/Tm = 0.000109 x (%1k in blend) + 0.0223, R2 = 0.97. A similar plot with data from the 3k/40k system yielded a non-linear relationship. Furthermore, the decrease in Tg for both 1k/100k and 3k/40k blends followed the Fox equation, although experimental values were consistently 1-2 degrees C above predicted values. Paclitaxel release from microspheres made with a 1k/100k blend occurred in four distinct phases: a burst phase (day 0), a slower phase, a second burst (day 35) and a second slower phase (until day 70). The seco...Continue Reading

References

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Citations

Feb 13, 2014·AAPS PharmSciTech·Susan D'SouzaPatrick P DeLuca
Jun 15, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Andrea MartinelliVincenzo Taresco
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Sep 22, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ashay JainGovind P Agrawal
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Sep 15, 2004·International Journal of Pharmaceutics·John K JacksonHelen M Burt
Apr 6, 2006·Journal of Biomedical Materials Research. Part a·Yuancai Dong, Si-Shen Feng
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Apr 28, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Hongshan LiangBin Li
Apr 8, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Yufei BianYang Li
Aug 9, 2020·International Journal of Nanomedicine·Avgi TsolouMaria D Koffa
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May 18, 2020·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Minh-Quan LeMarie-Claire Venier-Julienne
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