The b- and g-irradiation effects on stability of microspheres made of poly(lactide-co-glycolide) 50:50 copolymer (PLGA) containing bupivacaine (BU) were studied. Microspheres containing 10, 25, and 40% w/w, respectively, of BU were prepared by spray drying and irradiated in air with b- and g-irradiation at a dose of 25 kGy. Morphology (atomic force microscopy, particle-size analysis), physico–chemical characteristics (DSC and FT-IR spectroscopy), drug content and in vitro dissolution profile of microspheres were all determined; the stability of irradiated microspheres was evaluated over a 9-month period. The decrease of BU content in g-irradiated microspheres was almost always constant independent of the amount of BU per sample, therefore it was in inverse proportion to drug loading (range between 5 and 15%). BU release rate increased immediately after irradiation and increased slightly until 90 days of storage. As far as b-irradiated microspheres are concerned, BU content decreased in a significant way (¯3%) only in microspheres containing 10% w/w of BU. Immediately after irradiation, drug release rate in b-irradiated microspheres increased less than in the corresponding g-irradiated microspheres, and it did not change further over the following storage period. BU-loaded microspheres have been shown to be more stable against b- than g-irradiation. AFM revealed that the surface roughness of the irradiated microspheres increases depending on irradiation. As such, if a parameter is quantifiable, it is proposed as a marker of degradation due to ionizing radiation.

Poly(lactide-co-glycolide) microspheres containing bupivacaine: comparison between gamma and beta irradiation effects.

CONTI, BICE;GENTA, IDA;
2003-01-01

Abstract

The b- and g-irradiation effects on stability of microspheres made of poly(lactide-co-glycolide) 50:50 copolymer (PLGA) containing bupivacaine (BU) were studied. Microspheres containing 10, 25, and 40% w/w, respectively, of BU were prepared by spray drying and irradiated in air with b- and g-irradiation at a dose of 25 kGy. Morphology (atomic force microscopy, particle-size analysis), physico–chemical characteristics (DSC and FT-IR spectroscopy), drug content and in vitro dissolution profile of microspheres were all determined; the stability of irradiated microspheres was evaluated over a 9-month period. The decrease of BU content in g-irradiated microspheres was almost always constant independent of the amount of BU per sample, therefore it was in inverse proportion to drug loading (range between 5 and 15%). BU release rate increased immediately after irradiation and increased slightly until 90 days of storage. As far as b-irradiated microspheres are concerned, BU content decreased in a significant way (¯3%) only in microspheres containing 10% w/w of BU. Immediately after irradiation, drug release rate in b-irradiated microspheres increased less than in the corresponding g-irradiated microspheres, and it did not change further over the following storage period. BU-loaded microspheres have been shown to be more stable against b- than g-irradiation. AFM revealed that the surface roughness of the irradiated microspheres increases depending on irradiation. As such, if a parameter is quantifiable, it is proposed as a marker of degradation due to ionizing radiation.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/132407
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