Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation

Ravinder Verma,1 Ajeet Kaushik,2 Rafa Almeer,3 Md Habibur Rahman,4 Mohamed M Abdel-Daim,3,5 Deepak Kaushik1 1Department of Pharmaceutical Sciences, M.D. University, Rohtak, Haryana, 124001, India; 2NanoBioTech Laboratory, Health Systems Engineering, Department of Natural Sciences, Division of Scienc...

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Autores principales: Verma R, Kaushik A, Almeer R, Rahman MH, Abdel-Daim MM, Kaushik D
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Publicado: Dove Medical Press 2021
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spelling oai:doaj.org-article:f9d0829078de497188e33f60571637bc2021-12-02T14:18:39ZImproved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation1178-2013https://doaj.org/article/f9d0829078de497188e33f60571637bc2021-02-01T00:00:00Zhttps://www.dovepress.com/improved-pharmacodynamic-potential-of-rosuvastatin-by-self-nanoemulsif-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ravinder Verma,1 Ajeet Kaushik,2 Rafa Almeer,3 Md Habibur Rahman,4 Mohamed M Abdel-Daim,3,5 Deepak Kaushik1 1Department of Pharmaceutical Sciences, M.D. University, Rohtak, Haryana, 124001, India; 2NanoBioTech Laboratory, Health Systems Engineering, Department of Natural Sciences, Division of Sciences, Arts, & Mathematics, Florida Polytechnic University, Lakeland, FL, 33805-8531, USA; 3Department of Zoology, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia; 4Department of Pharmacy, Southeast University, Banani, Dhaka, 1213, Bangladesh; 5Pharmacology Department, Faculty of Veterinary Medicine, Suez Canal University, Ismailia, 41522, EgyptCorrespondence: Deepak KaushikDepartment of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, 124001, IndiaTel +91-931580962Email deepkaushik1977@gmail.comMohamed M Abdel-DaimDepartment of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi ArabiaEmail abdeldaim.m@vet.suez.edu.egPurpose: The purpose of this proposed research was to investigate a nano-formulation developed using self-nanoemulsifying drug delivery system (SNEDDS) to improve the pharmacodynamic potential of rosuvastatin by assisting its transportation through lymphatic circulation.Methods: The utilized lipids, surfactants, and co-surfactants for SNEDDS were selected on the basis of solubility studies. The SNEDDS formulation was optimized by implementing a D-optimal mixture design, wherein the effect of concentration of Capmul MCM EP (X1), Tween 20 (X2) and Transcutol P (X3) as independent variables was studied on droplet size (Y1), % cumulative drug release (Y2) and self-emulsification time (Y3) as dependent variables. The optimized formulation was evaluated via in vitro parameters and in vivo pharmacodynamic potential in Wistar rats.Results: The D-optimal mixture design and subsequent ANOVA application resulted in the assortment of the optimized SNEDDS formulation that exhibited a droplet size of nano range (14.91nm), in vitro drug release of > 90% within 30 minutes, and self-emulsification time of 16 seconds. The in vivo pharmacodynamic study carried out using Wistar rats confirmed the better antihyperlipidemic potential of developed formulation in normalizing the lipidic level of serum in contrast to pure drug and marketed tablets.Conclusion: This research reports the application of D-optimal mixture design for successful and systematic development of rosuvastatin-loaded SNEDDS with distinctly enhanced in vitro and in vivo performance in comparison to marketed formulation. Eventually, improved anti-hyperlipidemic efficacy was envisaged which might be attributed to increased drug solubility and absorption. Overall, this study shows the utility of SNEDDS for improving the dissolution rate and bioavailability of poor aqueous-soluble drugs. The present SNEDDS formulation could be a promising approach and alternative to conventional dosage form.Keywords: SNEDDS, rosuvastatin, in vitro lipolysis, nanotechnology, D-optimal mixture design, pharmacodynamic studyVerma RKaushik AAlmeer RRahman MHAbdel-Daim MMKaushik DDove Medical Pressarticlesneddsrosuvastatinin vitro lipolysisnanotechnologyd-optimal mixture designpharmacodynamic studyMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 905-924 (2021)
institution DOAJ
collection DOAJ
language EN
topic snedds
rosuvastatin
in vitro lipolysis
nanotechnology
d-optimal mixture design
pharmacodynamic study
Medicine (General)
R5-920
spellingShingle snedds
rosuvastatin
in vitro lipolysis
nanotechnology
d-optimal mixture design
pharmacodynamic study
Medicine (General)
R5-920
Verma R
Kaushik A
Almeer R
Rahman MH
Abdel-Daim MM
Kaushik D
Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
description Ravinder Verma,1 Ajeet Kaushik,2 Rafa Almeer,3 Md Habibur Rahman,4 Mohamed M Abdel-Daim,3,5 Deepak Kaushik1 1Department of Pharmaceutical Sciences, M.D. University, Rohtak, Haryana, 124001, India; 2NanoBioTech Laboratory, Health Systems Engineering, Department of Natural Sciences, Division of Sciences, Arts, & Mathematics, Florida Polytechnic University, Lakeland, FL, 33805-8531, USA; 3Department of Zoology, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia; 4Department of Pharmacy, Southeast University, Banani, Dhaka, 1213, Bangladesh; 5Pharmacology Department, Faculty of Veterinary Medicine, Suez Canal University, Ismailia, 41522, EgyptCorrespondence: Deepak KaushikDepartment of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, 124001, IndiaTel +91-931580962Email deepkaushik1977@gmail.comMohamed M Abdel-DaimDepartment of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi ArabiaEmail abdeldaim.m@vet.suez.edu.egPurpose: The purpose of this proposed research was to investigate a nano-formulation developed using self-nanoemulsifying drug delivery system (SNEDDS) to improve the pharmacodynamic potential of rosuvastatin by assisting its transportation through lymphatic circulation.Methods: The utilized lipids, surfactants, and co-surfactants for SNEDDS were selected on the basis of solubility studies. The SNEDDS formulation was optimized by implementing a D-optimal mixture design, wherein the effect of concentration of Capmul MCM EP (X1), Tween 20 (X2) and Transcutol P (X3) as independent variables was studied on droplet size (Y1), % cumulative drug release (Y2) and self-emulsification time (Y3) as dependent variables. The optimized formulation was evaluated via in vitro parameters and in vivo pharmacodynamic potential in Wistar rats.Results: The D-optimal mixture design and subsequent ANOVA application resulted in the assortment of the optimized SNEDDS formulation that exhibited a droplet size of nano range (14.91nm), in vitro drug release of > 90% within 30 minutes, and self-emulsification time of 16 seconds. The in vivo pharmacodynamic study carried out using Wistar rats confirmed the better antihyperlipidemic potential of developed formulation in normalizing the lipidic level of serum in contrast to pure drug and marketed tablets.Conclusion: This research reports the application of D-optimal mixture design for successful and systematic development of rosuvastatin-loaded SNEDDS with distinctly enhanced in vitro and in vivo performance in comparison to marketed formulation. Eventually, improved anti-hyperlipidemic efficacy was envisaged which might be attributed to increased drug solubility and absorption. Overall, this study shows the utility of SNEDDS for improving the dissolution rate and bioavailability of poor aqueous-soluble drugs. The present SNEDDS formulation could be a promising approach and alternative to conventional dosage form.Keywords: SNEDDS, rosuvastatin, in vitro lipolysis, nanotechnology, D-optimal mixture design, pharmacodynamic study
format article
author Verma R
Kaushik A
Almeer R
Rahman MH
Abdel-Daim MM
Kaushik D
author_facet Verma R
Kaushik A
Almeer R
Rahman MH
Abdel-Daim MM
Kaushik D
author_sort Verma R
title Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
title_short Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
title_full Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
title_fullStr Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
title_full_unstemmed Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation
title_sort improved pharmacodynamic potential of rosuvastatin by self-nanoemulsifying drug delivery system: an in vitro and in vivo evaluation
publisher Dove Medical Press
publishDate 2021
url https://doaj.org/article/f9d0829078de497188e33f60571637bc
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