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Issn: 2277–4998 IJBPAS, November, 2016, 5(11): 2986-3002 ISSN: 2277–4998 OPTIMIZATION, EVALUATION AND ANTIFUNGAL ACTIVITY DETERMINATION OF OXICONAZOLE LOADED TRANSFERSOMES GEL BY USING TEA TREE OIL KAUR N1*, GARG R2 AND DEVGAN M3 *1I.K. Gujral Punjab Technical University, Kapurthala, Jalandhar, Punjab-144601; 2Amar Shaheed Baba Ajit Singh Jujhar Singh Memorial College of Pharmacy, Bela 140111, Punjab, India 3 Faculty of pharmacy, RP educational trust group of institution, Bastara, Karnal *Corresponding author: #1079/12, Street no-7, shanti nagar Kurukshetra, Haryana-136119, Mb no.9017994328; Email: [email protected] th rd th st Received 27 July 2016; Revised 3 Sept. 2016; Accepted 28 Sept. 2016; Available online 1 Nov. 2016 ABSTRACT The main goal of present research work was to evaluate the oxiconazole (OXC) loading transfersomes gel by using tea tree oil. OXC loaded transfersomes formulation was optimized using central composite designs; where the effects of soya lecithin (SL): span80 (S80) molar ratio and the drug amount were evaluated by using variables; including vesicle size and drug entrapment efficiency (%EE). The optimized transfersomes formulation was ready with 85:15 SL: S80 molar ratio and 10 mg drug amount by using vortexing- sonication method with vesicle size of 1.47µm and %EE of 80.47±0.777%. The %Cumulative drug release of the optimized gel formulation (OXCG-6) through the cellophane membrane was excellent (87.891±0.314%) compared with other formulations. 2 The drug release kinetic obeys Higuchi model (R = 0.998 and Kh value 38.87) with fickian diffusion mechanism. The zone of inhibition of OXC transfersomes gel formulation (A) and liposome gel (B), plain gel (C) and marketed formulation (D) were found to be 28.6 ± 0.68, 20.2±0.39, 15.7 ± 0.41 and 19.4 ± 0.54 mm respectively against candida species. Results show that ‘A’ exhibits most antifungal activity after 24 h, So it can be concluded that the tea tree oil containing formulation ‘A’ exhibited better anticandidal activity than the other formulations. Results suggested transfersomes gel 2986 IJBPAS, November, 2016, 5(11) Kaur N et al Research Article containing tea tree oil to be the most conversant carrier system for transdermal delivery of OXC. Keywords: transfersomes, oxiconazole, tea tree oil, fungal infections INTRODUCTION Oxiconazole(1) (OXC) is 2,4-dichloro-2- Transfersomes can breach the skin barrier, (imidazol-1-yl) acetophenone O-(2,4 even through the pores that would be dichlorobenzyl) oxime is a confining for other particulates of synthetic imidazole derivative of a broad- comparable size(8). This capability is due spectrum antifungal activity and is used for to the extremely high deformability and topical treatment of topical fungal ultraflexible of the transfersomes infections(2). Ergosterol shows a hormone membrane(7). Because transfersomes are as role in fungal cells, which promote consisting of surfactant, they have better growth; the net efficacy of OXC is the elasticity and hydration properties, which inhibition the fungal growth(3). The OXC are credit for their superior skin penetration antifungal agents block the synthesis ability(9). Traditional liposomes are less of ergosterol is a major part of fungal deformable vesicles, are applied to the skin cytoplasmic membranes. Now today many surface where they dry completely and link, OXC formulations are available in the therefore they have less access power than market in the form of creams and lotions transfersomes(10). Transfersomes are but they show no retention properties in the combining of phospholipids, surfactant, and treatment of athlete's foot, tinea infection, water, make by thin film hydration(11), jock itch, candida(4) and in vaginal fungal vortexing-sonication method(12) and high infections. pressure homogenization method(13). Transfersomes(5) formulation is a good The focus of this research is to optimize, way to reduce above limitation. develop and evaluate the transfersomes Ultraflexible drug carriers(6) mainly vesicular carrier of OXC so as to provide retained at the place of administration the stable and to retain the anticandidal longer than liberated drug and efficient to activity of the drug by tea tree oil. Tea tree improve the dispersion of an concerned oil is here may be increases the antifungal substances and increase the efficacy and properties of OXC. It takes as important reduce toxicity. Gregor cevc was first role of natural penetration enhancer for introduced the word transfersomes (elastic improvement of antifungal properties of or ultraflexible liposomes)(7). drug. Further, they can be incorporated into 2987 IJBPAS, November, 2016, 5(11) Kaur N et al Research Article commonly used dermal vehicles, such as at room temperature for 6 h, for three carbopol gels, in order to have a right consecutive cycles. The suspension was semisolid consistency to facilitate easy skin extruded through 0.2 µm sartorius application producing high patient membrane filter (weender acceptance. landstr,goettingen Germany) for five times MATERIALS AND METHODS: at 50°C. Then transfersomes formulations Material: Oxiconazole (OXC) was were centrifuged in a refrigerated provided as a gift from A.S. Joshi and centrifuge (REMI Laboratory instruments, company Pvt. Ltd (Maharashtra, India). Tea thane, Maharashtra) for three hours at tree oil was purchased from Kanta 20,000 rpm and 4°C. OXC transfersomes at Enterprises Pvt. Ltd (Noida, India), the base of the tubes were cleaned with E Carbopol 940; Glycerin; and Cholesterol 7%v/v to remove the free drug and diluted (CL) was purchased from Hi-media labt. with E 7% (v/v) up to 10 ml. Samples were Pvt Ltd, (Mumbai). Span 80 (S80), Ethanol stored at 2-8°C in tightly closed containers (E) and Triethanolamine were purchased for further evaluations as shown in Table 1 from S.D. fine Chem Ltd (Mumbai). and in Table 2. Methanol and Dialysis membrane were Similarly, liposomes(14) (SL:CL, 70:30) of purchased from Hi-media labt. Pvt. Ltd OXC were prepared using cholesterol (Mumbai). Soya lecithin (SL) was instead of surfactants in the optimized purchased Titan biotech Ltd (Bhiwadi, formula as shown in Table 3. Rajasthan).Propylene glycol was purchased Experimental design: Central composite Central Drug House Ltd (New Delhi). designs were employed using Design- Methods: Transfersomes were prepared by Expert Software10.0.3.1.32-bit, using SL vortexing - sonication method(12). A and using S80. In these designs, two mixture of OXC, SL and S80 with different independent formulation variables were ratios was dissolved in 1ml of ethanol to prepensely to evaluate their combined form a solution. This mixture was dispersed effects and individualistic; SL:S80 molar in E 7% (v/v) (Ethanol) and vortexed for ratio (A) and amount of OXC added (B). 5min to attain a milky suspension. The The experimental trials were carrying out at suspension was sonicated by QSONICA all eight presumable combinations with 3 125 watt sonicator (M2 Scientifics times replication for each transfersomes Holland,Michigan) for 25 min followed by system(15). To study the effect of variables freezing at 15-20 °C for 12 h and thawing used central composite designs for 2988 IJBPAS, November, 2016, 5(11) Kaur N et al Research Article transfersomes performance and evaluation. way analysis of variance (ANOVA) was The central composite designs including applied to estimate the significance of the investigated independent and dependent model (P < 0.05) and particular response variables are shown in Table 2. The one- parameters. Table 1: Variables in central composite designs Level used -1 0 +1 Independent variables A: SL:S80(mg) 75:25 85:15 95:5 B: OXC(mg) 10 15 20 Dependent variables R1: Entrapment efficiency%(EE) R2: Vesicle size(µm) Table 2: Response parameters of transfersomes formulation of OXC prepared as per the experimental design Independent variable Dependant variables Formula A B EE% Vesicle size(µm) Code OXC-1 0 1 74.54±0.362 3.89±0.31 OXC-2 -1 1 59.52±0.538 4.07±0.930 OXC-3 -1 0 62.45±0.025 3.55±0.25 OXC-4 1 1 63.49±0.495 5.86±0.39 OXC-5 -1 -1 61.46±0.670 2.55±0.662 OXC-6 0 -1 80.47±0.777 1.47±0.110 OXC-7 1 -1 64.48±0.320 3.02±0.831 OXC-8 1 0 65.51±0.821 3.99±0.754 Each value represents the mean ± SD (N= 3) Table 3: Formulation of liposomes Batches SL: CL E E 7%v/v (ml) OXC (mg) EE (%) Vesicle size(µm) (mg) (ml) OXC-9 70:30 1 10 10 59.54±0.45 5.81±0.0251 Each value represents the mean ± SD (N= 3) Evaluation of vesicles: determined by an indirect method. The Morphological and size of vesicles: An vesicle solution was centrifuged (Remi optical microscope (Suswox 50ptic, Equipments, Mumbai, and India) at 10,000 sudheer scientific works, ambala cantt.) rpm at 4°C for 10 min. The combined fitted with a digital camera was used to supernatant was analyzed for the drug photograph the prepared formulation content after suitable dilution with blank before extrusion under magnification 40X. solution by measuring absorbance at 257 A fine layer of vesicles formulation was nm using UV Spectrophotometer spread on a glass slide and examined after (Systronics 2202, Ahmedabad). The placing the cover slip. The mean size of at supernatant was filtered and the least 100 particles was calculated. entrapment efficiencies of the OXC-loaded Entrapment efficiency: The entrapment formulation were calculated by (1). capacity of transfersomes vesicles was Entrapment efficiency% = (X1 – X2) ×1OO ……… (1) 2989 IJBPAS, November, 2016, 5(11) Kaur N et al Research Article X1 triethanolamine portion wise by sprinkling Where, to 10 ml of the previously prepared X1= Amount of OXC added initially, X2= Amount of OXC determined in the filtrate suspension of vesicles and stirring until a by spectrophotometrically, (X1 – X2) = represents the amount of OXC gel was formed (Table 4).
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