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Agrawal A.G.,Cachet Pharmaceutical Pvt. Ltd | Kumar A.,Cachet Pharmaceutical Pvt. Ltd
Archives of Pharmacal Research | Year: 2014

Coenzyme Q10 (CQ10) is known as an endogenous cellular antioxidant, naturally found in every cell of the human body and plays an important role in maintaining human health. It is widely used as a nutritional supplement and pharmaceutical drug for various disorders like diabetes mellitus, carcinomas, neurodegenerative disorders etc. However, CQ10 is practically insoluble even in the presence of 5 % sodium lauryl sulfate in water and poorly absorbed from the gastrointestinal tract. The present research is aimed to formulate and evaluate self nanoemulsifying drug delivery system (SNEDDS) of CQ10 primarily to improve its aqueous solubility, dissolution velocity as well as hepatoprotective activity and thus enhancing its nutraceutical and pharmaceutical values. Robustness to dilution, thermodynamic stability study, droplet size analysis and drug release were adopted to optimize liquid SNEDDS. Droplet size of the SNEDDS was found to be size less than 200 nm and appeared round in shape without aggregation under transmission electron microscopy examination. Liquid SNEDDS were adsorbed on porous carrier to get solid SNEDDS (S-SNEDDS). S-SNEDDS gave rapid (>90 %) drug release within 30 min while pure drug was not practically dissolved within 1 h. In vivo hepatoprotective activity showed that S-SNEDDS achieved the most liver protection as compared to the pure drug. Further S-SNEDDS was successfully converted to self nanoemulsifying mouth dissolving tablet. The enhanced solubility, dissolution velocity as well as hepatoprotective activity of CQ10, unravels the potential of S-SNEDDS as suitable carrier for enhancing nutraceutical and pharmaceutical values of CQ10. © 2014 The Pharmaceutical Society of Korea Source

Agrawal A.G.,Cachet Pharmaceutical Pvt. Ltd | Agrawal A.G.,Research and Development Cachet Pharmaceutical Pvt. Ltd | Kumar A.,Cachet Pharmaceutical Pvt. Ltd
Drug Research | Year: 2015

Recently within the lipid based formulation category, Self-nanoemulsifying drug delivery system (SNEDDS) has received considerable attention in the enhancement of bioavailability of poorly water-soluble drugs. Self-emulsifying formulation should have good solvent properties to allow appropriate solubility of the drug in the formulation. Drug incorporated in the formulation should also be readily dissolved as clear and monophasic liquid at ambient temperature when introduced to aqueous phase. N-methyl pyrrolidone (NMP) is one of the main pharmaceutical cosolvents and is a solubilizing excipient used in parenteral and oral medications. Marketed Leuprolide acetate (Sanofi-aventis, Quebec, Canada) is formulated as a solution composed of 55-66% NMP and 34-45% poly(DL-lactide-co-glycolide). Self-emulsifying oral formulation of fenofibrate containing NMP as solubilizer has been patented. Based on these reports we successfully developed SNEDDS formulation using NMP as cosolvent and found ~4 fold improvement in apparent permeability coefficient of model drug. To ensure the safety of the developed SNEDDS formulation, in the present study we further investigated its toxicity studies in mice and evaluated for various parameter. From the results it can be concluded that oral administration of SNEDDS formulation containing NMP did not exhibit significant toxicity in mice and further detail toxicity study is required so as to ensure the safety of this system in oral drug delivery. © Georg Thieme Verlag KG Stuttgart New York. Source

Agrawal A.G.,Cachet Pharmaceutical Pvt. Ltd | Kumar A.,Cachet Pharmaceutical Pvt. Ltd
Drug Development and Industrial Pharmacy | Year: 2015

Atorvastatin calcium (ATRC) is a poor water soluble drug used for treatment of hypercholesterolemia. This research is aimed to improve solubility and dissolution rate of ATRC by formulating into solid self-nanoemulsifying drug delivery system (S-SNEDDS) using N-methyl pyrrolidone (NMP) as cosolvent. Solubility of ATRC was determined in various vehicles. Ternary phase diagrams were constructed to identify stable nanoemulsion region. SNEDDS formulations were evaluated for robustness to dilution, thermodynamic stability study, % transmittance, self-emulsification time, globule size and transmission electron microscopy. The optimized liquid SNEDDS showed robust to all dilutions exhibiting no signs of phase separation or precipitation for 24 h. Liquid SNEDDS was transformed into S-SNEDDS using different adsorbents. Differential scanning calorimetry and scanning electron microscopy studies unravel the transformation of native crystalline state to amorphous state/solubilized state. In vitro dissolution study of S-SNEDDS was found to be significantly higher in comparison to that from plain drug, irrespective of pH (p < 0.001). Furthermore, ex vivo permeation studies showed a 4.45-fold improvement in apparent permeability coefficient (Papp) from S-SNEDDS compared to plain drug. In conclusion, S-SNEDDS prepared using NMP as cosolvent provides an effective approach for improved oral delivery of ATRC. © 2014 Informa Healthcare USA, Inc. Source

Agrawal A.G.,Cachet Pharmaceutical Pvt. Ltd | Kumar A.,Cachet Pharmaceutical Pvt. Ltd
Colloids and Surfaces B: Biointerfaces | Year: 2015

The aim of this study was to develop self emulsifying drug delivery systems (SEDDS) of glipizide and to convert it into solid SEDDS (S-SEDDS) using Syloid® 244 FP as adsorbent. Solubility study, ternary phase diagram, robustness to dilution, thermodynamic stability study and globule size analysis were adopted to optimize liquid SEDDS. S-SEDDS were evaluated for various studies including in vivo study. The optimized liquid SEDDS formulation consisted of phosphatidylcholine, Tween 80 and Transcutol P as oil, surfactant and cosolvent. In vivo study demonstrated that blood glucose levels were efficiently controlled with S-SEDDS compared with pure drug. The results of this study suggest the potential use of developed S-SEDDS formulation for the delivery of poorly water-soluble drug glipizide. © 2014 Elsevier B.V. Source

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