Nasal administration of heparin-loaded microspheres based on poly(lactic acid).
In this study, heparin-loaded microspheres having smooth surface and small particle size were designed in order to provide the absorption of heparin through nasal mucosa. For this purpose, microspheres at different polymer/drug ratios (1:10, 1:2.5 and 1:1) and at different concentrations of polyvinyl alcohol, emulsifying agent (1.5% and 2.5% w/v) were prepared by solvent evaporation method with poly(lactic acid). The microspheres were for evaluated shape and surface properties, particle size, production yield, encapsulation efficiency and in vitro drug release. Based on the in vitro data, selected microspheres were applied by nasal route to Wistar albino rats. According to in vivo studies, heparin-loaded microspheres may be used by nasal route as an alternative to parenteral route.
Yildiz
Ayca
A
Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Beyazt, 34116-Universite, Istanbul, Turkey.
Okyar
Alper
A
Baktir
Gül
G
Araman
Ahmet
A
Ozsoy
Yildiz
Y
D000281:Administration, Intranasal; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D001777:Blood Coagulation / Q000187:drug effects; D003692:Delayed-Action Preparations; D045703:Emulsifying Agents / Q000737:chemistry; D005260:Female; D006493:Heparin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019344:Lactic Acid / Q000737:chemistry; D008863:Microspheres; D009297:Nasal Mucosa / Q000378:metabolism; D010314:Partial Thromboplastin Time; D010316:Particle Size; D011091:Polyesters; D011108:Polymers / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013499:Surface Properties; D013696:Temperature
D000925:Anticoagulants; D003692:Delayed-Action Preparations; D045703:Emulsifying Agents; D011091:Polyesters; D011108:Polymers; D019344:Lactic Acid; C033616:poly(lactide); D011142:Polyvinyl Alcohol; D006493:Heparin