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Ultrafine super self-nano emulsifying drug delivery system of dolutegravir for improved dissolution rate

By: Gunaseelam, T. H.
Contributor(s): Habibur Rahman, S. M.
Publisher: M P BRNSS Publication Hub. 2021Edition: Vol.15(4), Oct-Dec.Description: 377-384p.Subject(s): PHARMACOGNOSYOnline resources: Click here In: International journal of green pharmacySummary: Aim: This work aimed to generate and evaluate different formulations of L-Self-nano emulsifying Drug Delivery System (SNEDDS) using different oil and Smix ratios to augment the dissolution rate of DTG. Methodology: L-SNEDDS of DTG was formulated with cinnamon oil and Capmul MCM as oil, TWEEN 80 as a surfactant, and PEG 400 as co-surfactant after preliminary screening using various vehicles for successful SNEDDS formulation. To optimize the system phase diagram was created and a self-nanoemulsifying region was identified. Sixteen formulations with various oil, surfactant, and co-surfactant ratios were produced and characterized concerning globule size, Polydispersity index (PDI), dispersibility, optical clarity, robustness to dilution, phase contrast microscopy, cloud point measurement, viscosity, thermodynamic stability study, and in vitro dissolution study. Results: The particle size of the F16 formulation was resolved to be 132.9 nm, with a PDI of 0.362, among the 16 formulations. Cinnamon oil and Capmul MCM were each 12.5 % of the F16 formulation, which also included 50 % tween 80 and 25% PEG 400. F16 was chosen as the optimum formulation, and it’s in vitro dissolution rate was compared to the marketed formulation and pure drug. In vitro dissolution studies of F16 (L-SNEDDS), Dolutegravir marketed tablet (DMT), and pure drug (DP) were compared, and it was found that the F16 formulation had the highest drug release of 96.68% at the end of 30 min, while the DMT and pure drug had 72.89% and 26.22%, respectively. Conclusion: The study revealed that the formulation of DTG as SNEDDS is a promising strategy to enhance the rate of dissolution.
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Aim: This work aimed to generate and evaluate different formulations of L-Self-nano emulsifying Drug Delivery System (SNEDDS) using different oil and Smix ratios to augment the dissolution rate of DTG. Methodology: L-SNEDDS of DTG was formulated with cinnamon oil and Capmul MCM as oil, TWEEN 80 as a surfactant, and PEG 400 as co-surfactant after preliminary screening using various vehicles for successful SNEDDS formulation. To optimize the system phase diagram was created and a self-nanoemulsifying region was identified. Sixteen formulations with various oil, surfactant, and co-surfactant ratios were produced and characterized concerning globule size, Polydispersity index (PDI), dispersibility, optical clarity, robustness to dilution, phase contrast microscopy, cloud point measurement, viscosity, thermodynamic stability study, and in vitro dissolution study. Results: The particle size of the F16 formulation was resolved to be 132.9 nm, with a PDI of 0.362, among the 16 formulations. Cinnamon oil and Capmul MCM were each 12.5 % of the F16 formulation, which also included 50 % tween 80 and 25% PEG 400. F16 was chosen as the optimum formulation, and it’s in vitro dissolution rate was compared to the marketed formulation and pure drug. In vitro dissolution studies of F16 (L-SNEDDS), Dolutegravir marketed tablet (DMT), and pure drug (DP) were compared, and it was found that the F16 formulation had the highest drug release of 96.68% at the end of 30 min, while the DMT and pure drug had 72.89% and 26.22%, respectively. Conclusion: The study revealed that the formulation of DTG as SNEDDS is a promising strategy to enhance the rate of dissolution.

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