|Year : 2012 | Volume
| Issue : 5 | Page : 116-117
Formulation of thermoresponsive and buccal adhesive in situ gel for treatment of oral thrush containing poorly water soluble drug bifonazole
Dimendra Patel1, Dipti Patel1, Jatin Prajapati1, Umang Patel1, Vijay Patel2
1 Deparatment of Pharmaceutics, Baroda College of Pharmacy, Limda, Vadodara, India
2 Deparatment of Pharmaceutics, Radhe College of Pharmacy, Vijapur, India
|Date of Web Publication||21-Mar-2012|
Deparatment of Pharmaceutics, Baroda College of Pharmacy, Limda, Vadodara
Source of Support: None, Conflict of Interest: None
| Abstract|| |
The aim of the present work is to formulate and evaluate in situ oral topical gels of poorly water soluble drug Bifonazole based on temperature induced systems for the treatment of oral candidiasis. Bifonazole is poorly water soluble and low permeable drug means it's belongs to BCS Class IV. Due to its poor water solubility, it necessary to enhance solubility in water by make complex with Beta- Cyclodextrin (Drug to βCyclo Dextrine ratio is 1:1). After in situ gel preparation done by using Poloxamer (10% and 15%w/w) along with carbopol 934 (0.2 to 1.0% w/w) and Bifonazole - β CD complex (1%w/w). The formulations were evaluated for physiochemical parameter, gelation Temperature, viscosity, gel strength, content uniformity mucoadhesive force, Diffusion Study.
Keywords: T0 emperature induced, topical in situ gel, oral candidiasis, bifonazole
|How to cite this article:|
Patel D, Patel D, Prajapati J, Patel U, Patel V. Formulation of thermoresponsive and buccal adhesive in situ gel for treatment of oral thrush containing poorly water soluble drug bifonazole. J Pharm Bioall Sci 2012;4, Suppl S1:116-7
|How to cite this URL:|
Patel D, Patel D, Prajapati J, Patel U, Patel V. Formulation of thermoresponsive and buccal adhesive in situ gel for treatment of oral thrush containing poorly water soluble drug bifonazole. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Jan 26];4, Suppl S1:116-7. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/116/94163
Candidiasis is an opportunistic infections condition caused by ubiquitous, saprophytic fungi of the genus Candida albicans.  Oral candidiasis is one of the most common pathological conditions affecting the oral mucosa . Bifonazole is Anti-fungal drug and its topical action and low systemic absorption. Bifonazole is poorly water soluble so solubility enhance by make complex with β Cyclo Dextrine (Drug to β Cyclo Dextrine ratio is 1:1).  Complex with β Cyclo Dextrine is prepared by Kneading Method. Poloxamer has temperature dependent gelling capacity. Poloxamer form solution at 2-5°C and Form gel at body temperature. 
| Materials and Methods|| |
Bifonazole were kindly gifted by vital health care (vapi), β Cyclo Dextrine, Carbopol 934, Poloxamer F-127, Methyl paraben.
Preparation of complex with β cyclo dextrine
Complex with β Cyclo Dextrine is prepared by Kneading Method. The calculated amounts of Bifonazole and CD were accurately weighed, transferred to a glass mortar, and triturated with a small volume of water/ethanol (1:1 volume ratio). The slurry obtained was kneaded for 30 min and then dried under vacuum at room temperature in the presence of calcium chloride as a dehydrating agent. Now this powder is use for preparation of in situ Gel.
Preparation of in situ gel
Different formulations were prepared with various ratios of Poloxamer F - 127 and Carbopol934 (10%, 15% w/w) : (0.2%, 0.6%, 1%w/w). The method involved slow addition Poloxamer F - 127and methyl paraben were solubilized in required quantity of cold distilled water (Sol. 1). Required quantities of Carbopol934 were kept overnight for swelling (Sol 2). Mix the both solution with continuous stirring (magnetic stir) until uniform solution obtained. After the mixture had been kept at ambient Temperature for 24 hrs a small amount of trienthanolamine was added to adjust the PH 7. An appropriate amount of Bifonazole - β CD complex dissolve in Cold water. This solution was added in polymer solution. Gel formation occurs at body temperature. Evaluated for various parameter.
| Results and Discussion|| |
It's temperature at which gel formation occurs. Viscosity of temperature induced gel formulation were increases with increase in concentration of Poloxamer F 127. (F1, F2 at 35 C, 24 C). In addition of carbopol 934 with Poloxamer F 127 ratio (10:0.2), (10:0.6), (10:1.03) And (15:0.2), (15:0.6), (15:1.0) it was found that the gradual increase in the gelation temperature of formulation (F3 to F8). So F1, F3, F7 and F8 is optimized batch [Table 1].
From viscosity study on optimized formulation showed increase in viscosity at 37°C. Addition of carbopol 934 (0.6% and 1.0%) increases in viscosity.
The percentage of drug diffused through chicken cheek mucous membrane over the period of 6hrs for formulation F1, F3, F7 and F8 was found to be 90.19%, 87.26%, 92.58%, 94.44%. The diffusion of drug from formulation F1 was less due to presence of poloxamer F 127 in the gel which retards the drug release rate owing to reduction in dimension of water channel. While diffusion of drug through formulation F3, F7 and F8 was found to be more due to presence of carbopol 934, which undergoes rapid swelling and helps in faster diffusion [Figure 1].
At 37°C, the gel strength of formulation F8 was found to be more than F7 and Gel strength of F3 was more than F1. This may be due to reversible gelation of poloxamer at 37°C [Table 2].
Mucoadhesive force of F1 is less compare to other due to absence of carbopol 934. Addition of carbopol 934 was increase mucoadhesive force of F3, F7, and F8 [Table 2].
pH of gel
All optimized formulation have pH range b/w 6.8 - 7.0.
| Conclusion|| |
It was seen that as the concentration of poloxamer F127 was increased the gelation temperature decreased. Carbopol 934 tends to increase the gelation Temperature of poloxamer F127. Thus from the above results it can be concluded that a temperature mediated in situ gelling mucoadhesive buccal gel of Bifonazole can be formulated using optimum quantity of poloxamer F127 and carbopol 934 combination of both to have a increase in Buccal residence time and patient comfort.
| Acknowledgement|| |
Authors would like to thank Vital health care (vapi) for providing Bifonazole as a gift sample and also thankful to Baroda college of pharmacy [Baroda] and Radhe college of pharmacy [Vijapur] for providing the facilities for the present work.
| References|| |
|1.||P. G. Fotos,S. D. Vincent and J. W Hallstein, Oral surg.med.oral patho.71 - 74. |
|2.||Uekama K, Hirayama F,Irie T. Cyclodextrin drug carrier systems. Chem Rev. 1998;98: 2045-2076. |
|3.||Sesai SD, Blanchard J. In-vitro evaluation of pluronic F-127 based controlled ocular delivery systems for pilocarpine. J. pharm. Sci., 1998, 87, 226-230. |
[Table 1], [Table 2]
|This article has been cited by|
||Preparation of fertility-promoting intrauterine infusion in situ gel and its in vitro release
| ||Lu, C.-C., Fu, H.-L., Zhou, T., Cao, H., Luo, L. |
| ||Guocheng Gongcheng Xuebao/The Chinese Journal of Process Engineering. 2014; 14(1): 139-144 |
||Critical Reviews in Therapeutic Drug Carrier Systems
| ||Wang, X., Liu, G., Ma, J.,Li, X., Zhang, Q. |
| ||In situ gel-forming system: An attractive alternative for nasal drug delivery. 2013; 30(5): 411-434 |