Investigation of enhancing effect of glucam® P-20 on the in vitro skin permeation of diclofenac sodium microemulsions

The aim of this work was to investigate the potential of Glucam® P-20 as a skin penetration enhancer for diclofenac sodium microemulsions across excised newborn pig skin. Glucam® P-20 (GP-20) or PPG-20-methyl glucose ether is generally used as a humectant, emollient and fragrance fixative. The w/o microemulsions composed of Tween 80, Eutanol G and water were formulated. The concentration of diclofenac sodium was 1 % w/w while the amounts of GP-20 were varied from 0-20 % w/w, ME-1 (0 %), ME-2 (5 %), ME-3 (10 %) and ME-4 (20 %). All microemulsions were transparent with Newtonian flow behaviour. The mean droplet sizes of the microemulsions were about 200 nm. The FTIR spectra of the microemulsions containing GP-20 were not markedly different from those of the microemulsion without GP- 20, ME-1. The in vitro release and skin permeation studies of diclofenac sodium loaded microemulsions were investigated using modified Franz diffusion cell. For the in vitro release across synthetic membrane, the rank order of the release rate was ME-4 > ME-3 > ME-2 > ME-1. For the in vitro skin permeation experiments, GP-20 at 10 % and 20 % could markedly enhance the percutaneous absorption of the drug. The optimum concentration of GP-20 was 10 %. GP-20 is proposed as a potential skin penetration enhancer for percutaneous absorption of diclofenac sodium.Colegio de Farmacéuticos de la Provincia de Buenos Aire

รายงานการวิจัยฉบับสมบูรณ์เรื่องการศึกษาสารเชิงซ้อนของ เบต้า-ไซโคลเด็กซ์ตรินกับน้ำมันตะไคร้หอมเพื่อไล่ยุง

Prince of Songkla University Faculty of Pharmaceutical Scienc

FORMULATION AND INVESTIGATION OF ANTIOXIDANT POTENTIAL OF O/W LOTIONS CONTAINING Tamarindus indica L. FRUIT PULP EXTRACT

The fruit pulp extracts of Tamarindus indica have been reported to possess several biological activities, especially antioxidant property which is suitable for cosmetic application. Therefore, the aims of this study were to formulate the tamarind fruit pulp extract loaded lotions (o/w emulsions), and to assess the antioxidant activity of tamarind fruit pulp extract loaded lotions. Initially, tamarind fruit pulp extracts were prepared by a solvent extraction method. The solvents used were water or a mixture of water and ethanol (water: ethanol= 1:1). Afterwards, the obtained tamarind fruit pulp extracts were subjected to lyophilization process. The tamarind fruit pulp extracts were tested for antioxidant activity by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay to determine suitable concentrations of the extracts to be incorporated into the lotions, which were 2 and 4%w/w in the current study. Apart from the basic ingredients of the oil phase and water phase, ViscOptima SE (2%w/w) was selected as an emulsifier and a thickener of the formulations. The tamarind fruit pulp extract loaded lotions were characterized for physicochemical property and antioxidant potential. The freshly prepared tamarind fruit pulp extract loaded lotions were light brown with homogeneity and no phase separation was observed after centrifugation at 3,000 rpm for 30 min. They had weak acidic pH (4.4-5.1), considered acceptable for skin application. The loaded formulations (F1, 2%w/w) and F2, 4%w/w)) exhibited significantly higher conductivity values than that of the unloaded formulation (F0) (p<0.05). The formulations behaved as pseudoplastic flows with low viscosity. The DPPH measurement revealed that the formulations F1 and F2 had potential antioxidant activity. In conclusion, topical o/w lotions containing tamarind fruit pulp extract were successfully prepared. They had substantial antioxidant activities. As a result, tamarind fruit pulp extract loaded lotions displayed a potential use in cosmetic formulations, especially antiaging products

Characterization, Antioxidant and Antibacterial Potentials of Tamarindus indica L. Fruit Pulp Extract Loaded O/W Nanoemulsions

The main purposes of the current study were to formulate o/w nanoemulsions as a carrier for Tamarindus indica (tamarind) fruit pulp extract and to study the antioxidant and antibacterial potentials of nanoemulsions containing tamarind extract, focusing on cosmetic/hygiene applications. The o/w nanoemulsions using a mixture of Tween 80 and Span 80 as an emulsifier (5%w/w) were prepared by a high pressure homogenization process. Two concentrations of sweet tamarind extract, 3.3 and 6.6%w/w, based on the bioactivity study, were incorporated into the blank nanoemulsions to produce loaded nanoemulsions, F1-3.3TE (3.3%) and F1- 6.6TE (6.6%). As compared with the unloaded nanoemulsion, both tamarind extract loaded nanoemulsions showed reduced pH and significantly increased viscosity. Overall, the loaded nanoemulsions had droplet sizes of approximately 130 nm, zeta potential around -38 mV and polydispersity index (PDI) values less than 0.2. The nanoemulsion F1-3.3TE had better stability (e.g. significantly greater % tartaric acid content and lesser PDI value) than the nanoemulsion F1-6.6TE did. The antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl assay revealed that the nanoemulsions F1-3.3TE and F1-6.6TE had scavenging activities of 81.66 ± 0.77% and 63.80 ± 0.79%, respectively. However, antioxidant activity of these two formulations decreased under stress conditions (heating-cooling cycles). Such incidence did not occur for their antibacterial properties investigated by agar well diffusion technique. The two formulations exhibited inhibition zones of approximately 24.0-27.7 mm against Staphylococcus aureus and Staphylococcus epidermidis, responsible for malodor of underarms. The results suggest the potential of using sweet tamarind pulp extract loaded nanoemulsions as hygiene products

Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

The objectives of this study were to develop and evaluate a novel self-emulsifying floating drug delivery system (SEFDDS) that resulted in improved solubility, dissolution, and controlled release of the poorly water-soluble tetrahydrocurcumin (THC). The formulations of liquid self-emulsifying drug delivery system (SEDDS; mixtures of Labrasol, Cremophor EL, Capryol 90, Labrafac PG) were optimized by solubility assay and pseudo-ternary phase diagram analysis. The liquid SEDDS was mixed with adsorbent (silicon dioxide), glyceryl behenate, pregelatinized starch, sodium starch glycolate, and microcrystalline cellulose and transformed into pellets by the extrusion/spheronization technique. The resulting pellets with 22% liquid SEDDS had a uniform size and good self-emulsification property. The microemulsions in aqueous media of different self-emulsifying floating pellet formulations were in a particle size range of 25.9–32.5 nm. Use of different weight proportions of glyceryl behenate and sodium starch glycolate in pellet formulations had different effects on the floating abilities and in vitro drug release. The optimum formulation (F2) had a floating efficiency of 93% at 6 h and provided a controlled release of THC over an 8-h period. The release rate and extent of release of THC liquid SEDDS (80% within 2 h) and self-emulsifying floating pellet formulation (80% within 8 h) were significantly higher than that of unformulated THC (only 30% within 8 h). The pellet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. Controlled release from this novel SEFDDS can be a useful alternative for the strategic development of oral solid lipid-based formulations