Abstract
Background and Objective: Applying Ethosomal Gels (EGs) in transdermal drug delivery systems has evoked considerable interest because of their good water-solubility and biocompatibility. The aim of present study was to prepare and characterize ethosomes of antileprotic drug Dapsone (DAP) together with an antibiotic Cloxacillin Sodium (CLXS) which may deliver these drugs to targeted site more efficiently than marketed gel preparation of DAP and also overcome the problems related with oral administration of CLXS. Methodology: Ethosomes were prepared by cold method then characterized for particle size, Entrapment Efficiency (EE), zeta potential and permeation studies. Vesicular size was determined by Scanning Electron Microscopy (SEM) and found to be varied from 127±9.01 to 215±7.23 nm depending on the concentrations of soya lecithin and ethanol. Results: The average percent drug entrapment efficiency of formulations ranged between 52.31% to 73.51% and 49.07% to 71.91% for DAP and CLXS respectively. The high ethanol concentration in ethosomes has shifted the vesicular charge from positive to negative. It was observed that F1 and F2 formulations were having zeta potential of -25.08±1.03 mV and -50.11±1.97 mV respectively and do not aggregate rapidly. The drug release of ethosomes ranged from 84.68% to 96.58% and 64.89% to 84.21% for DAP and CLXS respectively. Ethosomal gel was prepared with optimized ethosome and studied for its release and physicochemical characteristics. Conclusion: Finally, G5 demonstrated better (p < 0.05) antileprotic effect to improve effectiveness, stability and to reduce side effects and toxicity associated with the chosen drugs in order to treat Leprosy.
Highlights
IntroductionKnown as Hansen’s disease, is a worldwide health problem, varying from tuberculoid to Lepromatous Leprosy (i.e., paucibacillary to multibacillary disease) according to the host immune response
Leprosy, known as Hansen’s disease, is a worldwide health problem, varying from tuberculoid to Lepromatous Leprosy according to the host immune response
G5 demonstrated better (p < 0.05) antileprotic effect to improve effectiveness, stability and to reduce side effects and toxicity associated with the chosen drugs in order to treat Leprosy
Summary
Known as Hansen’s disease, is a worldwide health problem, varying from tuberculoid to Lepromatous Leprosy (i.e., paucibacillary to multibacillary disease) according to the host immune response. Since 1943, it has been the drug of choice in the treatment of leprosy because it has bacteriostatic action against Mycobacterium leprae by inhibiting folic acid production via competition with paminobenzoate for the active site of dihydropteroate synthase [2] It has obvious application in the field of dermatology, and may ease symptoms in diseases such as acne, Behçet’s disease, epidermolysis the bulbous acquisita, dermatitis herpetiformis, Kaposi’s sarcoma, and systemic lupus erythematosus [3]. CLXS, chemically monosodium (2S, 5R, 6R)-6-{[3-(2-chlorophenyl)-5-methyloxazole-4carbonyl] amino}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2- carboxylic acid is a semisynthetic antibiotic in the same class as penicillin It is the chlorinated derivative of ofloxacin and ofloxacin is used in the treatment of leprosy as an antibiotic drug. The aim of present study was to prepare and characterize ethosomes of antileprotic drug Dapsone (DAP) together with an antibiotic Cloxacillin Sodium (CLXS) which may deliver these drugs to targeted site more efficiently than marketed gel preparation of DAP and overcome the problems related with oral administration of CLXS
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