Preformulation Studies of Niosomal Gel of Prednisolone &Azithromycin

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Abstract Azithromycin is a semi-synthetic macrolide antibiotic drug, effective against a wide variety of bacteria. It is primarily used to treat the bacterial infections associated with weaker immune system. Prednisolone is a synthetic corticosteroid, used for suppressing the immune system and inflammation. When used in combination, both the drugs are very much effective in the management of inflammatory conditions or diseases in which the immune system plays an important role. The aim is to study the preformulation parameters for niosomal gel for topical use. The objective of Preformulation study is to generic information useful to the formulator in developing stable and bioavailable dosage form. The use of Preformulation parameter maximize the chances of getting a formulation which is safe, efficacious and stable product and at the same time provide optimization of the drug product quality. Administration of conventional tablets of prednisolone has been reported to exhibit delayed release and unwanted side effects so prednisolone loaded niosomes were developed and azithromycin which tend to cause allergic reaction was incorporated into gel base provide rapid penetration through skin , improve therapeutic performance, restrict action to the target cell and improve patient compliance, hence the objective of the study was made to develop sustained release gel containing azithromycin and niosomal vesicles of prednisolone using Carbopol as a polymer which will controlled the release of drug, increasing the bioavailability of the drug and thus decreasing the dosing frequency of the drug. The Preformulation studies were carried out for identification (physical appearance, melting point, and uv spectrophotometer), solubility profile, TLC, FTIR, compatibility studies, simultaneous estimation. All the observation and results showed that the azithromycin and prednisolone serve as suitable candidate for Topical drug delivery system that may improve the bioavailability. 1. Introduction Topical niosomal gel has been in use for dermatological disease since very long time. Azithromycin is a semisynthetic macrolide antibiotic drug, effective against a wide variety of bacteria. It is primarily used to treat the bacterial infections associated with weaker immune system. Prednisolone is a synthetic corticosteroid, used for suppressing the immune system and inflammation. When used in combination, both the drugs are very much effective in the management of inflammatory conditions or diseases in which the immune system plays an important role. The objective of Preformulation study is to generic information useful to the formulator in developing stable and bioavailable dosage form. The use of Preformulation parameter maximize the chances in formulation an safe, efficacious and stable product and compatible, at the same time provides simultaneous estimation studies and product quality. The Preformulation studies were carried out for identification (physical appearance, solubility studies, melting point, and uv spectrophotometer, IR spectra TLC, estimation of drugs). Niosomal gel has been explored extensively for Topical application to enhance skin penetration as well as skin retention of the drug. It provides effective and immediate release of the drugs. Prednisolone loaded niosomes were used to provide sustained release and protect the drug from external environment, which further are being evaluated before incorporating into gel base. 2. Materials and Method 1. Preformulation studies of drugs a) Azithromycin Solubility study of azithromycin was performed in 0.1 N HCl & water. Excess of AZI was dissolved separately in the above 2 solvents and shaken continuously for 24 hours in the mechanical shaker at 25±2°C. Solutions were filtered and absorbance was recorded using UV spectrometer and the amount of AZI dissolved in 10 ml of 0.1N HCl & water was calculated. Melting point The melting point of the drug was performed by capillary method. In this, drug was filled in the capillary tube sealed at one end to a height of 3 mm from closed end and capillary was introduced into digital melting point apparatus. The temperature range at which drug melt was noted down. IR Spectroscopy Characterization of AZI was done by FTIR spectroscopy. The drug was mixed with KBr & pressed into a very thin pellet which was then observed under IR spectrophotometer and the spectrum obtained was interpreted.