In vitro permeation characteristics of moxifloxacin from oil drops through excised goat, sheep, buffalo and rabbit corneas.
The objective of present investigation was to study the in vitro permeation characteristics of moxifloxacin from oil drops through freshly excised goat, sheep, buffalo and rabbit corneas. Moxifloxacin, 0.043 to 0.048% (w/v) ophthalmic solutions with or without (0.5% v/v) benzyl alcohol were made in arachis, castor, cottonseed, olive, soybean, sunflower and sesame oils. Permeation studies were conducted by putting 1 ml oil formulation on cornea (0.50 cm2) fixed between donor and receptor compartments of an all glass modified Franz diffusion cell and measuring the drug permeated in receptor (containing 10 ml bicarbonate ringer, pH 7.4 at 37 degrees C under stirring) by spectrophotometry at 291 nm, after 120 min. Post permeation corneal hydration was measured to assess corneal damage. The study was designed with paired corneas i.e. one cornea of an animal received formulation without benzyl alcohol while the contralateral cornea received formulation with benzyl alcohol. Moxifloxacin ophthalmic solution in castor oil showed maximum permeation with all the corneas. Addition of benzyl alcohol, a preservative, to oil drops reduced permeation of moxifloxacin from each oil drop, with corneas of all the species. Partition experiments with moxifloxacin oil drops and phosphate buffer (pH 7.4) indicated higher partitioning of drug in the oil phase, in presence of benzyl alcohol. Thus results of permeation are consistent with the partition characteristics of drug between oil and aqueous phase. Corneal hydration obtained with all the formulations was between 75 to 80% indicating no corneal damage.
Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences & Research, Formerly College of Pharmacy (University of Delhi), New Delhi, India.
P K
PK
Pawar
D K
DK
Majumdar
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D001372:Aza Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D001592:Benzyl Alcohols; D002020:Buffaloes; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003315:Cornea / Q000378:metabolism*; D024841:Fluoroquinolones; D006041:Goats; D066298:In Vitro Techniques; D000077266:Moxifloxacin; D009821:Oils; D010539:Permeability; D011804:Quinolines / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D012756:Sheep; D012996:Solutions
D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D001592:Benzyl Alcohols; D024841:Fluoroquinolones; D009821:Oils; D011804:Quinolines; D012996:Solutions; D000077266:Moxifloxacin