Date Published: June 30, 2017
Publisher: Tabriz University of Medical Sciences
Author(s): Swati Jagdale, Saylee Pawar.
Purpose: Ofloxacin is a fluoroquinolone with broad-spectrum antibacterial action, used in treatment of systemic and local infections. Ofloxacin is BCS class II drug having low solubility, high permeability with short half-life. The present work was aimed to design, develop and optimize gellified emulsion of Ofloxacin to provide site targeted drug delivery. Transdermal drug delivery will enhance the bioavailability of the drug giving controlled drug release.
Formulations that are applied to the skin or to mucus membrane are referred as transdermal or topical. Drugs administered through the topical route may have both local and systemic effects, depending on where the application is made and on how the formulation is been constructed. Three different functions may be achieved via application of the formulations to human skin.1 First function is the desirability to make the active remain on the surface of the skin, E.g. dermal insect repellents, skin infections, and cosmetics for skin decoration. These pharmaceuticals or cosmetics are called epidermal formulations. The second function is for those topical formulations which are designed for dermal penetration of their actives into the deeper regions of the skin such as the viable epidermis and dermis. These are called as endodermal or diadermal formulations. These formulations are not aimed to get absorbed into systemic circulation. Third function aimed to get the systemic action by transdermal application. Local reactions are undesired in this case. When a systemic effect is sought, topical administration can offer many advantages over oral or parenteral administration. The main advantage includes no first pass effect, the risks and inconveniences of parenteral administration are ignored and large variations in the pH in gastric emptying are avoided. Oppositely, if a local effect is sought; many adverse effects associated with an oral administration can be avoided when the topical route is used.2
Ofloxacin was gift sample from Mercury laboratories Ltd. HPMC K100M was a gift sample from Colorcon Asia Pvt. Ltd. Oleic acid and Span 80 were purchase from Merck specialties private Ltd. Tween 80 and propylene glycol 400 were obtained from Ranbaxy laboratories Ltd. Carbopol 940 was obtained from Analab fine chemicals. All other chemicals were of analytical grade.
Ofloxacin exhibited characteristic peaks as shown in Figure 1. One prominent characteristic peak was found in between 3050 and 3000 cm-1 which was assigned to stretching vibration of OH group and intramolecular hydrogen bonding. Band also suggested NH stretching vibration of the imino-moiety of piperazinyl groups which was less prominent due to intense OH stretching vibration. Peak at 2700 cm-1 indicated CH3 of methyl group. 1750-1700 cm-1 band represented the acidic carbonyl C=O stretching. 1650 to 1600 cm-1 peak was assigned to N-H bending vibration of quinolones. Band at 1550 to 1500 cm-1 represented CH2 of the aromatic ring. Band at 1450-1400 cm-1 indicated stretching vibration of CH2.This had confirmed presence of methylene group in benzoxazine ring. Peak at 1400-1350 cm-1 represented bending vibration of hydroxyl group. Band at 1250 to 1200 cm-1 suggested the stretching vibration of oxo group. In addition, a strong absorption peak between 1050 and 1000 cm-1 was assigned to C-F group. Band at 900-800 cm-1 represented the out of plane bending vibration of double bonded ‘enes’ or =CH groups (as per I.P.).
In conclusion, a stable, elegant and effective transdermal emulgel delivery for Ofloxacin has developed. The delivery was optimized using HPMC K100M and Carbopol 940 as a gelling agent. Emulgel exhibited good in-vitro drug release and viscosity. Emulgel will act as depot of drug which will release drug in controlled manner at the targeted site. Hence the optimized formulation F4 may be used to treat the topical bacterial diseases.
Authors are sincerely thankful to Mercury Laboratories Pvt. Ltd. for providing gift sample of drug. Authors would like to thank Colorcon Asia Pvt. Ltd., Mumbai, India for providing gift sample of HPMC. Authors are highly grateful to Dr. B. S. Kuchekar, Principal and management of MAEER’S Maharashtra Institute of Pharmacy, Pune, India for moral support and providing necessary infrastructure to carry out research work.
The authors declare no conflict of interests.