In vitro evaluation of pluronic F127-based controlled-release ocular delivery systems for pilocarpine.
The overall objective of this study was to develop pluronic F127 (PF127)-containing formulations of pilocarpine hydrochloride (PHCL) suitable for controlled-release ocular delivery of PHCL. Various aqueous formulations were evaluated containing 1% w/v PHCL and 25% w/v PF127 alone or with one of the following additives present: poly(ethylene glycol) 4600 (PEG), poly(vinylpyrrolidone) 10,000 (PVP), poly(vinyl alcohol) 10,000 (PVA), methylcellulose 15 cP (MC), and hydroxypropyl methylcellulose 80-120 cP (HPMC). The in vitro dissolution of the PF127 formulations and the pilocarpine release profiles from them were obtained simultaneously at 34 degrees C and room temperature using a membraneless in vitro model. It was observed that the PEG- and PVP-containing PF127 formulations of PHCL dissolved the quickest and released the drug at a significantly faster rate than the control PF127 formulation, which had no additive present. The PF127 formulations of PHCL containing MC or HPMC exhibited the slowest dissolution rates and released the drug the slowest. The same rank order was observed at each temperature for the dissolution and PHCL release profiles of each formulation. On the basis of the in vitro results, the PF127 formulations of PHCL containing MC or HPMC as an additive showed potential for use as controlled-release ocular delivery systems for PHCL.
Desai
S D
SD
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arizona, Tucson 85721, USA.
Blanchard
J
J
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D065347:Hypromellose Derivatives; D016018:Least-Squares Analysis; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008916:Miotics / Q000008:administration & dosage* / Q000737:chemistry; D009883:Ophthalmic Solutions; D010862:Pilocarpine / Q000008:administration & dosage* / Q000737:chemistry; D011060:Poloxalene / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D012212:Rheology; D014783:Viscosity
D003692:Delayed-Action Preparations; D005079:Excipients; D008916:Miotics; D009883:Ophthalmic Solutions; D010862:Pilocarpine; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D011060:Poloxalene; D008747:Methylcellulose; D011205:Povidone