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Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation.
Curr Drug Deliv. 2017; 14(7):1005-1015.CD

Abstract

PURPOSE

The objective of this study was to formulate and optimize Candesartan Cilexetil (CC) loaded nanostructured lipid carriers (NLCs) for enhanced oral bioavailability.

METHOD

Glycerol monostearate (GMS), Oleic acid, Tween 80 and Span 40 were selected as a solid lipid, liquid lipid, surfactant and co- surfactant, respectively. The CC-NLCs were prepared by hot emulsion probe sonication technique and optimized using experimental design approach. The formulated CC-NLCs were evaluated for various physicochemical parameters and further optimized formulation (CC-NLC-Opt) was assessed for in vivo pharmacokinetic and pharmacodynamic activity.

RESULTS

The optimized formulation (CC-NLC-Opt) showed particle size (183.5±5.89nm), PDI (0.228±0.13), zeta potential (-28.2±0.99mV), and entrapment efficiency (88.9±3.69%). The comparative in vitro release study revealed that CC-NLC-Opt showed significantly better (p<0.05) release and enhanced permeation as compared to CC-suspension. The in vivo pharmacokinetic study gave many folds increase in oral bioavailability than CC suspension, which was further confirmed by antihypertensive activity in a murine model.

CONCLUSION

Thus, the results of ex vivo permeation, pharmacokinetic study and pharmacodynamics study suggest the potential of CC-NLCs for improved oral delivery.

Authors+Show Affiliations

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, IndiaDepartment of Pharmaceutics, College of Pharmacy, Aljouf University, Sakaka, Aljouf, KSADepartment of Pharmaceutics, Glocal School of Pharmacy, The Glocal University, Sahararnpur, Uttar Pradesh, IndiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, IndiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, IndiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, IndiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, IndiaDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28034361

Citation

Paudel, Anjan, et al. "Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: in Vitro and in Vivo Evaluation." Current Drug Delivery, vol. 14, no. 7, 2017, pp. 1005-1015.
Paudel A, Ameeduzzafar , Imam SS, et al. Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation. Curr Drug Deliv. 2017;14(7):1005-1015.
Paudel, A., Ameeduzzafar, ., Imam, S. S., Fazil, M., Khan, S., Hafeez, A., Ahmad, F. J., & Ali, A. (2017). Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation. Current Drug Delivery, 14(7), 1005-1015. https://doi.org/10.2174/1567201813666161230141717
Paudel A, et al. Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: in Vitro and in Vivo Evaluation. Curr Drug Deliv. 2017;14(7):1005-1015. PubMed PMID: 28034361.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation. AU - Paudel,Anjan, AU - Ameeduzzafar,, AU - Imam,Syed Sarim, AU - Fazil,Mohd, AU - Khan,Shahroz, AU - Hafeez,Abdul, AU - Ahmad,Farhan Jalees, AU - Ali,Asgar, PY - 2016/07/26/received PY - 2016/10/25/revised PY - 2016/12/27/accepted PY - 2016/12/31/pubmed PY - 2018/6/29/medline PY - 2016/12/31/entrez KW - Antihypertensive activity KW - bioavailability study KW - candesartan cilexetil KW - formulation design KW - lipid formulation KW - nanoparticle SP - 1005 EP - 1015 JF - Current drug delivery JO - Curr Drug Deliv VL - 14 IS - 7 N2 - PURPOSE: The objective of this study was to formulate and optimize Candesartan Cilexetil (CC) loaded nanostructured lipid carriers (NLCs) for enhanced oral bioavailability. METHOD: Glycerol monostearate (GMS), Oleic acid, Tween 80 and Span 40 were selected as a solid lipid, liquid lipid, surfactant and co- surfactant, respectively. The CC-NLCs were prepared by hot emulsion probe sonication technique and optimized using experimental design approach. The formulated CC-NLCs were evaluated for various physicochemical parameters and further optimized formulation (CC-NLC-Opt) was assessed for in vivo pharmacokinetic and pharmacodynamic activity. RESULTS: The optimized formulation (CC-NLC-Opt) showed particle size (183.5±5.89nm), PDI (0.228±0.13), zeta potential (-28.2±0.99mV), and entrapment efficiency (88.9±3.69%). The comparative in vitro release study revealed that CC-NLC-Opt showed significantly better (p<0.05) release and enhanced permeation as compared to CC-suspension. The in vivo pharmacokinetic study gave many folds increase in oral bioavailability than CC suspension, which was further confirmed by antihypertensive activity in a murine model. CONCLUSION: Thus, the results of ex vivo permeation, pharmacokinetic study and pharmacodynamics study suggest the potential of CC-NLCs for improved oral delivery. SN - 1875-5704 UR - https://www.unboundmedicine.com/medline/citation/28034361/Formulation_and_Optimization_of_Candesartan_Cilexetil_Nano_Lipid_Carrier:_In_Vitro_and_In_Vivo_Evaluation_ L2 - https://www.eurekaselect.com/148832/article DB - PRIME DP - Unbound Medicine ER -