Formulation of a Novel Nanoemulsion System for Enhanced Solubility of a Sparingly Water Soluble Antibiotic, Clarithromycin

Abstract

The sparingly water soluble property of majority of medicinally significant drugs acts as a potential barrier towards its utilization for therapeutic purpose. The present study was thus aimed at development of a novel oil-in-water (o/w) nanoemulsion (NE) system having ability to function as carrier for poorly soluble drugs with clarithromycin as a model antibiotic. The therapeutically effective concentration of clarithromycin, 5 mg/mL, was achieved using polysorbate 80 combined with olive oil as lipophilic counterion. A three-level three-factorial central composite experimental design was utilized to conduct the experiments. The effects of selected variables, polysorbate 80 and olive oil content and concentration of polyvinyl alcohol, were investigated. The particle size of clarithromycin for the optimized formulation was observed to be 30 nm. The morphology of the nanoemulsion was explored using transmission electron microscopy (TEM). The emulsions prepared with the optimized formula demonstrated good physical stability during storage at room temperature. Antibacterial activity was conducted with the optimized nanoemulsion NESH 01 and compared with free clarithromycin. Zone of inhibition was larger for NESH 01 as compared to that with free clarithromycin. This implies that the solubility and hence the bioavailability of clarithromycin has increased in the formulated nanoemulsion system.

Evaluation of characterization and disinfection efficacy of chlorocresol nanoemulsion disinfectant

“…As shown in Table 5, KL of 0.06% CND were all more than 5 aer disinfecting respectively for 10 and 15 min, while KL of 0.06% chlorocresol aqueous solution were all less than 5 indicating disinfection disqualications. [22][23][24] In addition, it was reported that nanoemulsion structure itself had also extensive bactericidal activity. The result suggested that nanoemulsied disinfectant could improve efficacy against microorganism more than unemulsied disinfectant, which 21 The improvements in the efficacy of nanoemulsied drugs have also been reported.…”

Design and evaluation of oral nanoemulsion drug delivery system of mebudipine

“…An attractive aspect of O/W nanoemulsions is their ability to incorporate hydrophobic drugs into the oily phase, thereby enhancing their solubility (Vatsraj et al, 2014). Different oils were examined in solubility studies and Ethyl oleate was suggested as the best solvent for MB, thus, selected as our oily phase.…”

“…Since the solubility of a drug is the first step in oral absorption, low solubility can lead to a decreased bioavailability as well as high intra-and inter-individual variations in plasma (Stuchlik & Zak, 2001). Utilization of lipid formulations, such as nanoemulsions can help overcome this problem (Shen et al, 2011;Gorain et al, 2014;Vatsraj et al, 2014). Such improvements in bioavailability in drugs, formulated by lipid-or oil-based formulations may be explained by different mechanisms: decreased rate of gastric emptying, increased dissolution rate of the drug, increased solubility in the intestinal fluid and formation of lipoproteins that promote the lymphatic transport of highly lipophilic drugs have been suggested in the literature for this phenomenon (Gershanik & Benita, 2000).…”

Pharmacological studies on tetracycline and tetracycline nanoemulsion formulas. Mohamed S. Saber1, Aziza M. Amer2, Shymaa A. ElBadawy2, Mohamed M. Amer3, 1. PhD student in Pharmacol. , Vet. Service Division, Ministry of Defense, Egypt.. 2. 2. Dept. of Pharmacol., Facult. Vet. Med., Cairo University, Giza, Egypt. 3. 3. Dept. of Poult. Dis., Facult. Vet. Med., Cairo University, P.O. 12211, Giza, Egypt.

“…The active tetracycline in oil phase of oil-in-water nano-emulsion is protected from hydrolysis and oxidation [64,65]. WhileVatsraj et al [66] reported the solubility and the bioavailability of clarithromycin has increased in the formulated nanoemulsion system.Nanoemulsion as a drug delivery system improve bioavailability and pharmacokinetic activity of tetracycline [5][6][7][8][9][10][11]30,67].…”