title: Studies on ocular and parenteral application potentials of azithromycin- loaded anionic, cationic and neutral-charged emulsions.
abstract: Ocular and parenteral application potentials of azithromycin-containing, non-phospholipid-based cationic nanosized emulsion in comparison to the phospholipid-based anionic and neutral-charged nanosized emulsions were investigated. Various physical, chemical, nonclinical toxicity and antimicrobial activity studies (mean droplet diameter, surface charge, creaming index, entrapment efficiency, accelerated, long-term and freeze-thaw cycling stabilities, TLC study, modified hen's egg chorioallantoic membrane (HET-CAM) test, in vitro hemolysis test, in vitro and in vivo myotoxicity, and in vitro antimicrobial activity) were conducted for assessing the potentials of these three types of emulsions. Following autoclave sterilization, all of these emulsions exhibited a nanometer range mean particle diameter (200 ± 29 to 434 ± 13 nm). While the anionic and cationic emulsions did show high negative (-34.2 ± 1.23 mV) and positive zeta potential (42.6 ± 1.45 mV) values, the neutral-charged emulsion did not. Even with 5 freeze-thaw cycles, the cationic emulsion remained stable whereas other two emulsions underwent phase-separation. The hen's egg chorioallantoic membrane test revealed an irritation score value that was higher for the anionic emulsion than for cationic or neutral-charged emulsion. A significantly higher % hemolysis value was also noticed for the anionic emulsion when compared to the % hemolysis value of cationic emulsion (ANOVA, P ‹ 0.05). However, all of the emulsions showed a lesser intracellular creatine kinase (CK) release/plasma CK level in comparison to the positive control (phenytoin) indicating their lesser myotoxicity at the injection site . When compared to anionic and neutral-charged emulsions, the possible controlled drug release from cationic emulsion delayed the in vitro antimicrobial action against H.influenzae and S.pneumoniae.
authors.affiliation: Department of Pharmaceutics, Lovely School of Pharmaceutical Sciences, Lovely Faculty of Applied Medical Sciences (LFAMS), Lovely Professional University, Phagwara- 144402, Jalandhar, Punjab, India.. tamilvanan2k@yahoo.com.
authors.forename: Shunmugaperumal
authors.initials: S
authors.lastname: Tamilvanan
authors.forename: Ramona
authors.initials: R
authors.lastname: Khanum
authors.forename: Sudalimuthu Ramachandran
authors.initials: SR
authors.lastname: Senthilkumar
authors.forename: Marimuthu
authors.initials: M
authors.lastname: Muthuraman
authors.forename: Thenrajan
authors.initials: T
authors.lastname: Rajasekharan
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry; D017963:Azithromycin / Q000008:administration & dosage* / Q000737:chemistry; D002645:Chickens; D049033:Chorioallantoic Membrane / Q000187:drug effects / Q000473:pathology; D003402:Creatine Kinase / Q000378:metabolism; D004355:Drug Stability; D004655:Emulsions; D004912:Erythrocytes / Q000187:drug effects / Q000473:pathology; D006193:Haemophilus influenzae / Q000187:drug effects / Q000254:growth & development; D006461:Hemolysis / Q000187:drug effects; D006470:Hemorrhage / Q000139:chemically induced; D007263:Infusions, Parenteral; D008055:Lipids / Q000737:chemistry; D008297:Male; D018482:Muscle, Skeletal / Q000187:drug effects / Q000378:metabolism; D020442:Poloxamer / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012756:Sheep; D013296:Streptococcus pneumoniae / Q000187:drug effects / Q000254:growth & development; D013499:Surface Properties
chemical_list: D000900:Anti-Bacterial Agents; D004655:Emulsions; D008055:Lipids; D020442:Poloxamer; D017963:Azithromycin; D003402:Creatine Kinase