Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability

DOI:

https://doi.org/10.37285/ijpsn.2015.8.4.1

Authors

  • Kishan V
  • Usha Kiranmai Gondrala
  • Narendar Dudhipala

Abstract

Felodipine is an antihypertensive drug with poor oral bioavailability due to the first pass metabolism. For improving the oral bioavailability, felodipine loaded solid lipid nanoparticles (SLNs) were developed using trimyristin, tripalmitin and glyceryl monostearate. Poloxamer 188 was used as surfactant. Lipid excipient compatibilities were confirmed by differential scanning calorimetry. SLN dispersions were prepared by hot homogenization of molten lipids and aqueous phase followed by ultrasonication at a temperature, above the melting point. SLNs were characterized for particle size, zeta potential, drug content, entrapment efficiency and crystallinity of lipid and drug. In vitro release studies were performed in 0.1N HCl and phosphate buffer of pH 6.8 using dialysis method. Pharmacokinetics of felodipine-SLNs after oral admini-stration in male Wistar rats was studied. The bioavailability of felodipine was increased by 1.75 fold when compared to that of a felodipine suspension.

 

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Keywords:

Solid-lipid nanoparticles, felodipine, lipophilic, bioavailability, pharmacokinetics.

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Published

2015-11-30

How to Cite

1.
V K, Gondrala UK, Dudhipala N. Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability. Scopus Indexed [Internet]. 2015 Nov. 30 [cited 2024 Jun. 20];8(4):2995-3002. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/803

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Section

Research Articles

References

Bhanu PS and Malay KD (2014). Nanosuspension for enhancement of oral bioavailability of felodipine. Appl Nanosci, 4: 189-197.

Capewell S, Freestone S, Critchlev JA, Pottage A and Prescott LF (1988). Reduced felodipine bioavailability in patients taking anticonvulsants, Department of clinical pharmacology, Royal Infirmary, Edinburgh. Lancet, 27 (2): 480-2.

Cavalli R, Bargoni A, Podio V and Muntoni E (2003). Duodenal administration of solid lipid nanoparticles loaded with different percentages of tobramycin. J Pharm Sci, 92(5): 1085-1094.

Charman WN and Porter CJH (1996). Lipophilic prodrugs designed for intestinal lymphatic transport. Adv Drug Deliv Rev, 19(2): 149-169.

Driscoll MC (2002). Lipid-based formulations for intestinal lymphatic delivery. Eur J Pharm Sci, 15: 405-415.

Harivardhan Reddy L and Murthy RSR (2005). Etoposide loaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release and stability evaluation. AAPS Pharm Sci Tech, 6(2): E158–E166.

Heitai H, Tawashi R and Philips NC (1998). Drug retention and stability of solid lipid nanoparticles containing azidothymidine palmitate after autoclaving, storage and lyophilization. J Microencapsul, 15(2): 173-84.

Holm R, Mullertz A, Pedersen GP and Christensen HG (2001). Comparison of the lymphatic transport of halofantrine administered in disperse systems containing three different unsaturated fatty acids. Pharm Res, 18(9): 1299-1304.

Jenning V and Gohla S (2000). Comparison of wax and glycerides solid lipid nanoparticles. Int J Pharm, 196(2): 219-222.

Manjunath K and Venkateswarlu V (2005). Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J Contr Rel, 107: 215-228.

Mansbach CM and Nevin P (1998). Intracellular movement of triacylglycerols in intestine. J Lipid Res, 39(5): 963-968.

Mehnert W and Mäder K (2001). Solid lipid nanoparticles production, characterization and applications. Adv Drug Deliv Rev, 47: 165-196.

Müller RH, Mäder K and Gohla S (2000). Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art, Eur J Pharm Biopharm, 50: 161-177.

Narendar D and Kishan V (2014). Candesartan cilexetil loaded solid lipid nanoparticles for oral delivery: characterization, pharmacokinetic and pharmacodynamic evaluation. Drug Delivery, Early Online: 1-10. DOI: 10.3109/10717544.2014. 914986.

Nordskog BK, Phan CT, Nutting DF and Tso P (2001). An examination of the factors affecting intestinal lymphatic transport of dietary lipids. Adv Drug Deliv Rev, 50(1-2): 21-44.

Porter CJH and Charman WN (2001). Intestinal lymphatic drug uptake: an update. Adv Drug Deliv Rev, 60(6): 61-80.

Pradeep RP, Shailesh VB and Anant RP (2009). Extended release felodipine self-nanoemulsifying system. AAPS Pharm Sci Tech, 10(2): 515-23.

Ros E (2000). Intestinal absorption of triglyceride and cholesterol, dietary and pharmacological inhibition to reduce cardiovascular risk. Atherosclerosis, 151(2): 357-379.

Shah U, Joshi G and Sawant K (2014). Improvement in antihyper-tensive and antianginal effects of felodipine by enhanced absorption from PLGA nanoparticles optimized by factorial design. Mater Sci Eng C Mater Biol Appl, 35(1): 153-63.

Suvarna G, Narender D and Kishan V (2015). Preparation, Characterization and In vivo Evaluation of Rosuvastatin Calcium Loaded Solid Lipid Nanoparticles. Int J Pharm Sci Nanotech, 8(1): 2779-2785.

Venkateswarlu V and Manjunath K (2004). Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles, J Contr Rel, 95(3): 627-638.

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