Abstract

AZITHROMYCIN-A NOVEL DRUG DELIVERY SYSTEM FOR OCULAR APPLICATION

Dinesh P. Kawade*, Rahul H. Kasliwal and Dinesh R. Chaple

Abstract

Azithromycin (AZT) is a macrolide antibiotic derived from and similar in structure to erythromycin. Oral administration of AZT is effective for the treatment of trachoma; however, topical formulations are difficult to develop because of the drug's hydrophobicity. The aim of this study is to formulate a novel topical ophthalmic delivery system of AZT. A major problem being faced in ocular therapeutics is the attainment of an optimal concentration at the site of action. Poor bioavailability of drugs from ocular dosage forms is mainly due to the tear production, nonproductive absorption, transient residence time, and impermeability of corneal epithelium. In addition to this, drugs that are hydrophobic or unstable at the pH comfortable in eye cannot be formulated as eye drops. Novel drug delivery systems could be some effective means of exploring the potential of such drugs.[1-4] The treatment of ocular surface infections with topical AZT is desirable in medicine because systemic exposure to the drug is limited.[7] Major topical formulation problems arise from the fact that AZT is hydrophobic and sparingly soluble in water at neutral pH.[5] Therefore, there is a need to design a novel drug delivery system, which could deliver the drug topically. Ocular inserts are polymeric systems into which the drug is incorporated as a solution (hydrophilic drug) or dispersion (hydrophobic drug) and molded as solid or semi-solid sterile preparations, of appropriate size and shape, designed to be inserted behind the eyelid or held on the eye and to deliver drugs for topical or systemic effect.

Keywords: Azithromycin, Macrolide, Novel drug delivery system, Ocular application.