Double-walled microspheres loaded with meglumine antimoniate: preparation, characterization and in vitro release study

作者:Navaei Ali; Rasoolian Morteza*; Momeni Arash; Emami Shahriar; Rafienia Mohammad
来源:Drug Development and Industrial Pharmacy, 2014, 40(6): 701-710.
DOI:10.3109/03639045.2013.777734

摘要

Objective: The objective of this study was to fabricate double-walled poly(lactide-co-glycolide) (PLGA) microspheres to increase encapsulation efficiency and avoid rapid release of hydrophilic drugs such as meglumine antimoniate. %26lt;br%26gt;Methods: In this study, double-walled and one-layered microspheres of PLGA were prepared using the emulsion solvent evaporation technique to better control the release of a hydrophilic drug, meglumine antimoniate (Glucantime (R)), which is the first choice treatment of cutaneous leishmaniasis. The effect of hydrophobic coating on microspheres%26apos; size, morphology, encapsulation efficiency and drug release characteristics was evaluated. Furthermore, the presence of antimony in meglumine antimoniate made it possible to observe the drug distribution within the microspheres%26apos; cross section by means of energy dispersive X-ray spectroscopy. %26lt;br%26gt;Results: Drug distribution images confirmed accumulation of the drug within the inner core of double-walled microspheres. In addition, these microspheres encapsulated the drug more efficiently up to 87% and demonstrated reduced initial burst and prolonged release compared to one-layered microspheres. These superiorities make double-walled microspheres an optimum candidate for sustained delivery of hydrophilic drugs. %26lt;br%26gt;Conclusion: Double-walled microspheres provide some advantages over traditional microspheres overcoming most of their limitations. Double-walled microspheres were found to be more efficient than their corresponding one-layered microspheres in terms of encapsulation efficiencies and release characteristics.

  • 出版日期2014-6