Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.
The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.
Department of Pharmaceutics, KLE University College of Pharmacy, JN Medical College Campus, Belgaum, 590010, Karnataka, India. bknanjwade@yahoo.co.in
Basavaraj K
BK
Nanjwade
Rucha V
RV
Deshmukh
Kishori R
KR
Gaikwad
Kemy A
KA
Parikh
F V
FV
Manvi
D060433:Administration, Ophthalmic; D000464:Alginates / Q000737:chemistry; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D001372:Aza Compounds / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D016503:Drug Delivery Systems; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients / Q000737:chemistry*; D024841:Fluoroquinolones; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D020100:Hydrogels; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D000077266:Moxifloxacin; D044367:Phase Transition; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011804:Quinolines / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D011817:Rabbits; D013696:Temperature; D013997:Time Factors; D014783:Viscosity
D000464:Alginates; D000890:Anti-Infective Agents; D001372:Aza Compounds; D005079:Excipients; D024841:Fluoroquinolones; D006603:Hexuronic Acids; D020100:Hydrogels; D011804:Quinolines; D020442:Poloxamer; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D020723:Glucuronic Acid; D008747:Methylcellulose; D000077266:Moxifloxacin