Characterization of crosslinked high amylose starch matrix implants. 1. In vitro release of ciprofloxacin.
The objective of this study was to characterize in vitro the potential of crosslinked high amylose starch (CLHAS) as an implant matrix for the delivery of ciprofloxacin (CFX). Direct compression of dry blends of four different matrices: control CLHAS; CLHAS with 1% hydrogenated vegetable oil (HVO); and CLHAS with 10 or 20% hydroxypropylmethylcellulose (HPMC), each of them with three CFX loadings (2.5, 5.0 and 7.5%) was performed to prepare twelve implant formulations. All CLHAS implants were used for 24-h dissolution tests to evaluate swelling, erosion, water uptake and CFX release. Additionally, 1%-HVO- CLHAS implants were used for an extended dissolution test. The presence of HPMC in the matrix increased CFX release rate, swelling, erosion and water uptake in a concentration-dependent manner whereas HVO had no effect. With increasing drug loading, a decrease of cumulative CFX percent release was observed in both 24-h and extended dissolution tests. Of the different formulations tested, CLHAS implants with 1% HVO and 7.5% CFX provided the longest period of drug delivery without any initial burst effect.
Désévaux
Cyril
C
Faculty of Pharmacy, University of Montreal, C.P. 6128, Succ. Centre-ville, Montreal (QC), H3C 3J7, Canada. cyril.desevaux@umontreal.ca
Dubreuil
Pascal
P
Lenaerts
Vincent
V
D000688:Amylose / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002939:Ciprofloxacin / Q000737:chemistry*; D003432:Cross-Linking Reagents / Q000737:chemistry*; D004339:Drug Compounding; D004343:Drug Implants / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D010938:Plant Oils / Q000737:chemistry; D013213:Starch / Q000737:chemistry*; D013997:Time Factors
D003432:Cross-Linking Reagents; D004343:Drug Implants; D005079:Excipients; D010938:Plant Oils; D065347:Hypromellose Derivatives; D002939:Ciprofloxacin; D008747:Methylcellulose; D013213:Starch; D000688:Amylose