FORMULATION AND IN-VITRO EVALUATION OFNAIL LACQUER CONTAINING FLUCONAZOLE FOR PREUNGUAL DRUG DELIVERY
MASTER OF PHARMACY DISSERTATION PROTOCOL
SUBMITTED TO THE
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,
BANGALORE.
BY
Ms. SAWANT DESSAI AMRITA RAMCHANDRA
M.PHARM – I
Under The Guidance of
Mr. SHRIPATHY D. M. Pharm.
ASST. PROFESSOR
DEPARTMENT OF PHARMACEUTICS.
SRINIVAS COLLEGE OF PHARMACY, VALACHIL MANGALORE – 574143.
2012-2014
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES
BANGALORE, KARNATAKA
ANNEXURE-II
PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION
1. / NAME OF THE CANDIDATE AND ADDRESS: / Ms.SAWANT DESSAI AMRITA RAMCHANDRA.1st M.PHARM,
DEPARTMENT OF PHARMACEUTICS
SRINIVAS COLLEGE OF PHARMACY,
VALACHIL, MANGALORE-574143.
2. / NAME OF THE INSTITUTION: / SRINIVAS COLLEGE OF PHARMACY,
VALACHIL, MANGALORE-574143.
3. / COURSE OF STUDY AND SUBJECT: / MASTER OF PHARMACY (PHARMACEUTICS)
4. / DATE OF ADMISSION: / 26/05/2012
5. / TITLE OF THE PROJECT:
“FORMULATION AND IN-VITRO EVALUATION OF NAIL LACQUER CONTAINING FLUCONAZOLE FOR PREUNGUAL DRUG DELIVERY”
6.
7. / Brief resume of intended work:
6.1 – Need of the study:
Over the last decades the treatment of illness has been accomplished by administrating drugs to human body via various routes namely oral, parental, topical, inhalation etc.1 Topical delivery of systemic therapeutics offer benefits but presents a great technical challange. The benefits include first pass avoidance, convenience and sustained release.
The topical formulations conventionally used in dermatology (creams, oil-based lotions, powders) are not specifically adapted to the nail since they are readily removed by rubbing, whipping, and washing; and their impermanence at the site of application readily accounts for their inefficacy.2
Conventional nail lacquers have been used as cosmetics since a long time for beautification and protection of nails. Nail lacquer can be used as a drug delivery system for the drugs that exhibit poor oral bioavailability.2
Medicated nail lacquer are formulations that are used for transungual drug delivery system for maximal antifungal efficacy.1 However improvement in the topical delivery of compounds for treatment of nail fungal diseases would reduce the need for systemic administration of drugs with its associated side effect.2Medicated nail lacquer are specially designed for the nail. These preparations are generally used in fungal diseases. Use of this system avoids systemic toxicity of fungal drugs.The film on the nail surface acts as a drug depot that permits optimized and sustained diffusion across the nail and leads to continuous penetration of active principle to high tissue concentration required for the efficacy for the treatment for nail fungal diseases.1
Onychomycosis is an infection of the nail caused by fungi such as dermatophytes, non-dermatophytes moulds and yeast (mainly Candida species). Of these 80% of the toenail infections are caused by dermatophytes (Trychophytonrubrum)3.
Fluconazole is chemically 2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)-2-propanol, asynthetic triazole derivative antifungal agent that has been shown to be effective against a widerange of systemic and superficial fungal infections, following both oral and intravenousadministration. Fluconazole, a novel bis‐triazole antifungal agent, hassystemic effects that may be beneficial for other fungal infections.4
The present invenstigation is aimed at formulation and evaluation of nail lacquer containing Fuconazolefor treatment of onychomycosis.
6.2 – Review of literature:
Literature survey was carried out on the proposed topic using Internet, RGUHS (Helinet Consortium) and referring journals.
- Patel RP, Naik SA, Patel NA, Suthar AM, reviewed the anatomy of a human nail, diseases related to nail plate, the formulations designed for nail application and some techniques used to enhance the topical bioavailability of the drugs across the nail, latest trends in drug delivery across the nail.5
- Tandel A, Agrawal S, Wankhede S,have formulated and evaluated the transungual permeation of the Voriconazole nail lacquer against Trichophyton Rubrum. The formulation was prepared using different polymers like cellulose nitrate, disodium hydrogen phosphate etc. The permeability studies were performed to determine the amount of voriconazole permeated in the nail. They concluded that permeability of voriconazole increased in the presence of thioglycollic acid.6
- Shireesh KR, Chandra SB, Vishnu P, Prasad MVV, have formulated and evaluated Ketoconazole nail lacquer for the treatment of onychomycosis. The permeability of the nail lacquer is increased by using different permeation enhancers like thioglycollic acid, urea hydrogen peroxide etc.the formulation is also evaluated for different parameter. It was found that thioglycollic acid increased the permeability of ketoconazole as compared to urea hydrogen peroxide.7
- Rajendra VB, Baro A, Kumari A, Dhamecha DL, Lahoti SR, Shelke SD, have studied the structure of the nail and different infectious conditions affecting it. They also carried out studies on different other parameters like permeation studies and methods to increase the permeation across the nail. They concluded that the delivery of the drug across highly karitinized tissue is difficult and can be increased by ungual and transungual delivery through the nail. The permeability of the drug can be enhanced by using permeation enhancers.8
- Alam G, Singh MP, Singh A, Vishwakarma DK, Patel R, Srivastava SP,have studied different disorders of the nail along with the physiology of the nail. They concluded the significance of the ungual and transungual drug delivery system. And showed that these routes of administration can be made effective by using appropriate concentration of the drug and penetration enhancers.9
- Mitkari BV, Korde SA, Mahadik KR, Kokare CR, formulated and evaluated liposomal gel for topical use containing Fluconazole. The liposome were prepared by film hydration technique using carbopol and evaluated. They concluded that the variable amount of the phospholipid, stabiliser have profound effect on the vesicle size and entrapment efficacy.10
1) To formulate nail lacquer containing Fuconazole with different penetration enhancers.
2) To check drug excipients compatibility by FTIR.
3) To evaluate physicochemical parameters of prepared nail lacquer.
4) To carry out in vitro permeation studies.
5) To carry out stability studies as per ICH guidelines.
Materials and Method:
Materials:
- Drug: Fluconazole
- Permeation enhancers: Urea H2O2 Thioglycolic Acid, DMSO etc.
- Excipients: Propylene Glycol, Glycerine, Ethanol & Polyethylene Glycol 400 etc.
8. / 7.1 – Source of data:
Review of literature
1)Journals:
International Journal of Current Pharmaceutical Research.
Asian Journal of Pharmaceutics.
International Journal of Applied Pharmaceutics.
Journal of Pharmacy Research
Journal of Drug Delivery and Therapeutics
2)Internet browsing.
3)Laboratory based studies.
7.2 – Method of Collection of Data:
- Formulation of nail lacquer.
- Evaluation of nail lacquer:
Drying time2, 7
Smoothness of flow2, 7
Gloss2, 7
In- vitro studies2, 7
- Across artificial membrane
- Transungual permeation studies
Conducted on patients or other humans or animals? If so, please describe
briefly.
Not Applicable.
7.4 – Has ethical clearance been obtained from your institution in case of 7.3?
Not Applicable.
List of references:
- Suryavanshi KA, Basru PR, Katedeshmukh RG. Review on Nail Transungual Drug Delivery System. Am. J. PharmTech Res. 2012;2(5):222-04.
- Sabreen J, Divyakumar B, Kiran B. Preungual drug delivery systems of terbinafine hydrochloride nail lacquer. Asian J Pharm 2008;02:53-06.
- Shirwaikar AA, Thomas TA, Lobo R, Prabhu KS. Treatment of Onychomycosis: An Update. Ind J Pharm Sci 2008 Nov-Dec;70(6):710-14.
- Lalit SK, Panwar SA, Darwhaker G, Jain DK. Formulation and Evaluation of Fluconazole Amphiphilogel.Der Pharmacia Lettre, 2011; 3 (5):125-31.
- Patel RP, Naik SA, Patel NA, Suthar AM. Drug delivery across human nail. Int J Curr Pharm Res 2009;01:01-07.
- Tandel A, Agrawal S, Wankhede S. Transungual Permeation Of The Voriconazole Nail Lacquer Against Trichophyton Rubrum. J Drug Delivery & Therapeutics 2012;2(1):25-33.
- Shireesh KR, Chandra SB, Vishnu P, Prasad MVV. Ungual Drug Delivery System Of Ketoconazole Nail Lacquer. Int J Appl Pharm 2010;2(4):17-19.
- Rajendra VB, Baro A, Kumari A, Dhamecha DL, Lahoti SR, Shelke SD. Transungual Drug Delivery: An Overview. J Appl Pharm Sci 2012;2(1):203-09.
- Alam G, Singh MP, Singh A, Vishwakarma DK, Patel R, Srivastava SP. Trans-ungual drug transport: advancement and challenges. J Pharm Res 2012;5(5):2574-79.
- Mitkari BV, Korde SA, Mahadik KR, Kokare CR. Formulation and evaluation of liposomal gel for fluconazole. Ind J Pharm Educ Res 2010;44(4):324-33.
9. /
Signature of candidate
/ (Amrita Ramchandra Sawant Dessai)10. /
Remarks of the guide
/ The work, which is assigned to Ms. Sawant Dessai Amrita Ramchandra is under my guidance.11. /
11.1 Name and Designation of the Guide
/ Mr. SHRIPATHY D. M.PharmAsst. Professor
Department of Pharmaceutics
Srinivas college of Pharmacy
Valachil, Mangalore-574143.
11.2 Signature
11.3 Name and Designation of Co-Guide
/ ------11.4 Signature
/ ------11.5 Head of Department
/ Dr. A. R. SHABARAYA M.Pharm., Ph.D.HOD and Principal
Department of Pharmaceutics
Srinivas College of Pharmacy,
Valachil, Mangalore- 574143
11.6 Signature
/ (Dr. A. R. Shabaraya.)12. /
12.1 Remarks of the Principal
/ Recommended and forwarded for favourable considerations.12.2 Signature
/ Dr. A. R. SHABARAYA M.Pharm, Ph.D.Director and Principal
Srinivas College of Pharmacy
Valachil, Mangalore- 574143