Enhanced oral bioavailability of salmeterol by loaded PLGA microspheres: preparation, in vitro, and in vivo evaluation.
The objective of the current study was to prepare microspheres of salmeterol (SM) using poly (lactide-co-glycolide) (PLGA) and assess its viability to enhance the oral bioavailability. Microspheres of SM were prepared by oil-in-water emulsion-solvent evaporation method. The formulations were characterized in encapsulation efficiency, particle size, zeta potential, and in vitro release. The prepared microspheres were found to be spherical in shape with smooth surface. The size of microspheres ranged from 14.7 to 16.5 µm. The polydispersity index (PDI) was 0.12 ± 0.05 and the zeta potential was -33.2 ± 1.4 mV. In vitro release profile, SM was graduated released from the microspheres as time lapsed, suggesting that SM was well entrapped in SM-loaded PLGA microspheres. The model that fitted best for SM released from the microspheres was Higuchi equation. In vivo study, SM-loaded PLGA microspheres are thought to have the potential to maintain SM concentration within target ranges for a long time, decreasing side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency.
a Oncology Department of Shanghai Pulmonary Hospital , Tongji University School of Medicine , Shanghai , China.
Haiping
H
Zhang
a Oncology Department of Shanghai Pulmonary Hospital , Tongji University School of Medicine , Shanghai , China.
Jianfang
J
Xu
D061605:Administration, Intravenous; D000284:Administration, Oral; D000318:Adrenergic beta-Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004655:Emulsions; D005079:Excipients; D019344:Lactic Acid / Q000737:chemistry; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D000068299:Salmeterol Xinafoate / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012995:Solubility
D000318:Adrenergic beta-Agonists; D004655:Emulsions; D005079:Excipients; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000068299:Salmeterol Xinafoate
PLGA microspheres; Pharmacokinetics; release; salmeterol