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  • After the comparison of surface mesh property

    2018-10-25

    After the comparison of surface mesh property of the designed molecules and three dimensional mesh structure of the active site it can be concluded that, there is a large extent of similarity between them. This similarity can be a major reason for active binding of the designed ligands with the receptor protein (Fig. 2). It was also noticed that the binding pattern of the designed molecules at the receptor active site is appreciably similar with that of WR99210. Binding energy of the designed molecule suggests that they are more tightly bound with the active site SB 431542 as compared to WR99210. The molecules were found to interact with key amino acids viz. Asp 54, Phe 58, Ile 164, Ser 108, Ser 111, Thr 185 (Table 5), Fig. 3.
    Acknowledgement Financial support for this work from the DBT, Govt. of India (DBT/330/NE/TBP/2012 dated 9th April 2013) is gratefully acknowledged. Authors also acknowledge the support obtained from SAIF NEHU for MS and NMR Spectroscopy.
    Introduction Desonide have been extensively used against inflammatory and pruritic diseases with dermatose infection as it possess glucocorticoid potency [1–3]. Desonide is effectively used to cure redness, swelling, itching and discomfort of diverse skin conditions. Desonide have a vital place as topical corticosteroids [4]. Chemically, it is (11β, 16α)-11, 21-Dihydroxy-16, 17-[(1-methylethylidene) bis (oxy)] pregna-1, 4-diene-3, 20-dione (Fig. 1) [1]. Desonide is constitutent of many lotion, cream, gel, ointment, foam and hydrogel as a topical formulation in the market. With reference to the present literature, numerous analytical methods are reported for the estimation of desonide in lotion, ointment and biological fluids. The literature reveals the development of HPLC method for assay of desonide in lotion and ointment [5,6], SIAM [7] photostability of desonide lotion [6,7] and analysis of its degradation product in ointment [8]. Few researchers have developed ESI-LC-MS/MS method based on principle of pH extraction and HPLC-mass spectrometry for identification and confirmation of doping agents in urine samples [9,10]. S-Lau et al. reported the GLC method for analysis of hydrocortisone, triamcinolone acetonide and desonide in mouse and human dermal fibroblasts culture media [11]. In 2008, Vonaparti et al. developed two simple and rapid LC/MS methods for the quantification and identification of hydrocortisone in equine urine using ion trap mass spectrometry (IT-MS) and time-of-flight mass spectrometry (TOF-MS) [12]. Afterwards, in 2005, Pujos et al. made comparison between developed ELISA, GC and LC method for analysis of some endogenous and synthetic corticosteroids including desonide [13]. One more analytical method also reported by UV spectrophotometer [14].
    Experimental
    Forced degradation study In oxidative degradation study, about 10 mg desonide was dissolved in 10 mL methanolic solution of hydrogen peroxide (1%, v/v). The solution was refluxed at 70 °C for 30 min in dark so as to exclude the possible degradative effect of light. The resultant solution (600 ng/band) was applied on a TLC plate in triplicate.
    Results and discussion
    Conclusion
    Acknowledgments We are thankful to Glenmark Pharmaceutical Ltd, Nashik, (India) for providing gift sample of desonide for research purpose. We would also like to extend our thanks to Dr. S. J. Surana Sir, Principal, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur for providing research facilities to carry out this project work.
    Introduction The topical drug delivery system offers major obstacle of low diffusion rate of drug across the skin. Several strategies were proposed to increase permeation of drugs across the membrane. One of the most promising strategies is vesicle based permeation [1–9,16]. Vesicles in topical drug delivery can be used as permeation enhancer, deliver entrapped drug through skin and act as rate limiting membrane barrier and modulate systemic absorption.