Bhalerao et al Journal of Drug Delivery & Therapeutics. 2019; 9(3):212-221 ISSN: 2250-1177 [212] CODEN (USA): JDDTAO Available online on 15.05.2019 at http://jddtonline.info Journal of Drug Delivery and Therapeutics Open Access to Pharmaceutical and Medical Research © 2011-18, publisher and licensee JDDT, This is an Open Access article which permits unrestricted non-commercial use, provided the original work is properly cited Open Access Research Article Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension Bhalerao Aparna 1 *, Choudhari Pankaj 2 1 JSPM’s Charak College of Pharmacy and Research, Wagholi, Pune, Maharashtra-412207 2 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 Article Info: Received 24 March 2019; Review Completed 03 May 2019; Accepted 06 May 2019; Available online 15 May 2019 Cite this article as: Bhalerao A, Choudhari P, Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension, Journal of Drug Delivery and Therapeutics. 2019; 9(3):212-221 http://dx.doi.org/10.22270/jddt.v9i3.2849 *Address for Correspondence: Dr Aparna V. Bhalerao, Associate Professor, JSPM's Charak College of Pharmacy and Research, Wagholi, Pune, Maharashtra, India-412207 INTRODUCTION Hypertension also called a silent killer is one of the most important risk factors for cardiovascular disease, a leading cause of death 1 . Various classes of a drug as diuretics, α- blockers, b-blockers, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II type 1 receptor blockers (ARB), and organic calcium channel blockers (CCBs) are used alone or in combination for the treatment of hypertension. Short- acting calcium channel antagonists decrease the blood pressure by vasodilation but are unable to decrease the blood pressure associated with sympathetic overactivity which is a secondary to the vasodilation 1,2 . To lessen or avoid the neurohormonal activation caused by short-acting calcium channel blockers (CCB), fourth generation dihydropyridine (DHP) based N and L-type calcium channel antagonists like cilnidipine have been developed that have potential clinical benefits: gradual onset of action and a long duration of effects along with renal protection by decreasing the activity of the sympathetic nervous system (SNS) and the renin-angiotensin system 2,3,4 . Cilnidipine is highly lipophilic, BCS class II drug with very low water solubility, which limits the dissolution rate of cilnidipine in water and in turn oral bioavailability. All calcium channel blocker undergoes extensive hepatic first-pass metabolism 5 , and are also substrates for p-glycoprotein resulting in limited oral bioavailability. Solid lipid nanoparticles(SLN) dissolve the lipophilic drug in lipid which protects the drug from enzymatic degradation and facilitates the transport of drug through lymphatic route thus avoids the hepatic first pass metabolism 6,7,8 . MATERIAL AND METHODS Cilnidipine was obtained as gift sample from JB Chemical, Mumbai, India Labrafil 1944, Compritol, Precirol were obtained as gift samples from Gattefosse Corporation, France, poloxamer 407 was obtained from BASF India, oleic acid, Tween 20, Tween 80, propylene glycol, polyethylene glycol, Span 60, isopropyl myristate, ethyl oleate, isopropyl palmitate, and glyceryl monostearate, were purchased from Research Lab Ltd. All other chemicals used were of analytical grade.