In situ gelling xyloglucan formulations for sustained release ocular delivery of pilocarpine hydrochloride.
Thermoreversible gels formed in situ by aqueous solutions of an enzyme-degraded xyloglucan polysaccharide were evaluated as sustained release vehicles for the ocular delivery of pilocarpine hydrochloride. In vitro release of pilocarpine from gels formed by warming xyloglucan sols (1.0, 1.5 and 2.0% w/w) to 34 degrees C followed root-time kinetics over a period of 6 h. The miotic responses in rabbit following administration of xyloglucan sols were compared with those from in situ gelling Pluronic F127 sols and from an aqueous buffer solution containing the same drug concentration. Sustained release of pilocarpine was observed with all gels, the duration of miotic response increasing with increase of xyloglucan concentration. The degree of enhancement of miotic response following sustained release of pilocarpine from the 1.5% w/w xyloglucan gel was similar to that from a 25% w/w Pluronic F127 gel.
Miyazaki
S
S
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, 061-0293, Hokkaido, Japan.
Suzuki
S
S
Kawasaki
N
N
Endo
K
K
Takahashi
A
A
Attwood
D
D
D000818:Animals; D003692:Delayed-Action Preparations; D005079:Excipients; D005782:Gels; D005936:Glucans; D008916:Miotics / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D009883:Ophthalmic Solutions; D010862:Pilocarpine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D020442:Poloxamer; D011134:Polysaccharides / Q000737:chemistry*; D011680:Pupil / Q000187:drug effects; D011817:Rabbits; D014783:Viscosity; D014990:Xylans
D003692:Delayed-Action Preparations; D005079:Excipients; D005782:Gels; D005936:Glucans; D008916:Miotics; D009883:Ophthalmic Solutions; D011134:Polysaccharides; D014990:Xylans; D010862:Pilocarpine; D020442:Poloxamer; C029353:xyloglucan