Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

  • Aparna Bhalerao JSPM’s Charak College of Pharmacy and Research, Wagholi, Pune, Maharashtra-412207
  • Pankaj Prakash Chaudhari Micro Labs Limited, Chandivali, Andheri East, Mumbai, Maharashtra-400072

Abstract

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine.


Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

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Author Biographies

Aparna Bhalerao, JSPM’s Charak College of Pharmacy and Research, Wagholi, Pune, Maharashtra-412207

JSPM’s Charak College of Pharmacy and Research,  Wagholi, Pune, Maharashtra-412207

Pankaj Prakash Chaudhari, Micro Labs Limited, Chandivali, Andheri East, Mumbai, Maharashtra-400072

Micro Labs Limited, Chandivali, Andheri East, Mumbai, Maharashtra-400072

References

1. Uneyama H, Uchida H, Konda T, Yoshimoto R. Cilnidipine: Preclinical profile and clinical evaluation. Cardiovascular drug reviews. 1999; 17(4):341-57.
2. Sakaki T, Naruse H, Masai M, Takahashi K, Ohyanagi M, Iwasaki T, Fukuchi M. Cilnidipine as an agent to lower blood pressure without sympathetic nervous activation as demonstrated by iodine-123 metaiodobenzylguanidine imaging in rat hearts. Annals of nuclear medicine. 2003; 17(4):321-6.
3. Chandra KS, Ramesh G. The fourth-generation Calcium channel blocker: cilnidipine. Indian heart journal. 2013; 65(6):691-5.
4. Aritomi S, Koganei H, Wagatsuma H, Mitsui A, Ogawa T, Nitta K, Konda T. The N-type, and L-type calcium channel blocker cilnidipine suppresses renal injury in Dahl rats fed a high-salt diet. Heart and vessels. 2010; 25(6):549-55.
5. Liu XQ, Zhao Y, Li D, Qian ZY, Wang GJ. Metabolism and metabolic inhibition of cilnidipine in human liver microsomes. Acta Pharmacologica Sinica. 2003; 24(3):263-8.
6. Youssef T, Fadel M, Fahmy R, Kassab K. Evaluation of hypericin-loaded solid lipid nanoparticles: Physicochemical properties, photostability, and phototoxicity. Pharmaceutical development and technology. 2012; 17(2):177-86.
7. Houli L, Zhao X, Ma Y et al. Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles. Journal of Controlled Release. 2009; 133:238-44.
8. Xia Q, Hao X, Lu Y, Xu W, Wei H, Ma Q, Gu N. Production of drug-loaded lipid nanoparticles based on phase behaviors of special hot microemulsions. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2008; 313:27-30.
9. Subedi RK, Kang KW, Choi KH. Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin. European Journal of Pharmaceutical Science.2009; 37:508-513.
10. Luo YF, Chen DW, Ren LX, Zhao XL, Qin J. Solid lipid nanoparticles for enhancing vinpocetine's oral bioavailability. Journal of controlled release. 2006; 114(1):53-9.
11. Rachmawati H, Rasaputri DH, Tarini S. Preparation and Characterization of Folic Acid-Encapsulated. Journal NANOSAINS & NANOTEKNOLOGI. 2010; 3(2):37-40.
12. Xia Q, Lu YY, Gu N. Preparation of lipid nanoparticles based on phase behaviors of hot microemulsions. In Solid State Phenomena. 2007; 121:847-50.
13. Prabakaran L, Remya B. Formulation and characterization of Domperidone solid lipid nanoparticles in an aqueous system using micro emulsification technique. Journal of Pharmacy Research.2010; 3(12):2944-46
14. Serpe L, Canaparo R, Daperno M et al. Solid lipid Nanoparticles as anti-inflammatory drug delivery system in human inflammatory bowel disease whole- blood model. European J of Pharmaceutical Sci. 2010; 39:428-36
15. Li HL, Zhao XB, Ma YK, Zhai GX, Li LB, Lou H. Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles. Journal of Controlled Release. 2009; 133(3):238-44
16. Severino P, Andreani T, Macedo A et al. Current State-of-Art and New Trends on Lipid Nanoparticles (SLN and NLC) for Oral Drug Delivery. Journal of Drug Delivery.2011; 2012:1-6
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How to Cite
Bhalerao, A., & Chaudhari, P. (2019). Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension. Journal of Drug Delivery and Therapeutics, 9(3), 212-221. https://doi.org/10.22270/jddt.v9i3.2849