Formulation and Characterization of Eye Drops Containing Microsphere of Acyclovir against Herpes Simplex Induced Keratitis

Pharmacy

Novel Drug Delivery System promotes the importantly ease and convenience of administration, deliverance of accurate dose as well as to prolong residence time of drug in contact with eye, that problems generally encountered in semisolid dosage forms. During the Preformulation studies it is found that the organoleptic properties of acyclovir comply as reported. White crystalline, tasteless, odorless, substance was sparingly soluble in water but dispersible. Five different formulations were prepared all the sodium alginate solutions were prepared by dissolving the respective amounts in distilled water. Dried microspheres were subjected for Evaluation were found yield between 83.68 to 92.02%, mean particle size between 583.34 to 816.21µm and % encapsulation between 78. 15 to 93.36% and swelling Index between 3.85 to 4.58 and shape was spherical with slightly elongated tips found in some microspheres. All microsphere formulations give more than 79 % drug release in steady way. All prepared microsphere formulations were tested In-vitro Drug Release and % drug release found as P-1(82.72), P-2(81.82), P-3(83.51), P-4(95.82) and P-5(89.15). On the basis of % drug release regression coefficient of P-4 was found greater (R² = 0.966), hence, P-4 is the best formulation having maximum % of drug release (95.82%) also selected for further studies. Formulated microsphere preparations were incorporated in eye drop suspension comprises of crystalline methyl cellulose as thickening agent, Boric acid as Buffering agent, Sodium chloride as Tonicity modifier, Sodium metabisulphate as Antioxidant, Benzalkonium chloride as Preservative and Sterile water as Vehicle. That eye drop suspensions were evaluated and found all formulations were clear, odorless, homogeneous and free from grittiness and also controlled pH between 7.1-7.8. Only batch F-5 was found irritant because of higher concentration of surfactant. In-vitro drug release data of Optimized formulation F-4 was subjected for kinetic modeling. Best fitted models are zero order, first order and Korsmeyer –Peppas model with R2 of 0.998.

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