Solid Lipid Nanoparticles

A Synopsis on “Formulation, development & evaluation of Solid Lipid Nanoparticles of Adapalene” submitted to NIMS UNIVERSITY, Shobha Nagar, Jaipur : 

A Synopsis on “Formulation, development & evaluation of Solid Lipid Nanoparticles of Adapalene” submitted to NIMS UNIVERSITY, Shobha Nagar, Jaipur IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE DEGREE OF “MASTER OF PHARMACY” (PHARMACEUTICS) SUBMITTED BY MANMOHAN UNDER THE GUIDANCE OF: Mr. Tarkeshwar Prasad Shukla Ms. Mithilesh Singh Asstt. Professor Asstt. Professor Deptt. of Pharmaceutics Deptt. of Pharmachemistry Guide Co-guide

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CONTENTS INTRODUCTION DRUG PROFILE REVIEW OF LITERATURE OBJECTIVE OF WORK PLAN OF WORK REFERENCES

INTRODUCTION: 

INTRODUCTION

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Solid lipid nanoparticles (SLNs) are submicron colloidal carriers (50-1000 nm) which are composed of physiological lipids, dispersed in water or in an aqueous surfactant solution . Several types of colloidal drug delivery including solid lipid nanoparticles (SLNs), liposome, dendrimers, and polymeric nanoparticles [1] systems have been developed:- to improve the specific delivery of drug to improve absorption of poorly water-soluble molecules protect sensitive active molecules against in-vivo degradation modify the distribution of drugs in the body increase the patient’s comfort by avoiding side effects.

ADVANTAGES OF NANOPARTICLES:: 

ADVANTAGES OF NANOPARTICLES: Site specific drug delivery. Controlled release of active drug over a long period can be achieved. Protection of incorporated drug against chemical degradation. Incorporation of drug can reduce distinct side effects of drug.

DRUG PROFILE: 

DRUG PROFILE

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Name: Adapalene Brand Names: Adaferin, Differin IUPAC Name: 6-[3-(1-adamantyl)- 4-methoxyphenyl] naphthalene-2-carboxylic acid Chemical Formula: C 28 H 28 O 3 Drug Category: Non-Steroidal Anti-Inflammatory Agents and Dermatological Agents Molecular Weight: 412.52 Structure:

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Mechanism of action: adapalene binds to specific retinoic acid nuclear receptors, it is suggested that topical adapalene may normalize the differentiation of follicular epithelial cells resulting in decreased microcomedone formation. State : Solid . Solubility: Insoluble in water, soluble in tetrahydrofuran, sparingly soluble in ethanol. Dose: 1-3mg/ gm Half-life: 0.8-2.4 hrs. Storage: Store at controlled room temperature ( 20 °-25°C )

REVIEW OF LITERATURE: 

REVIEW OF LITERATURE

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Bhalekar et. al. (2009) , prepared compritol-888-ATO-based SLN dispersions containing Miconazole having low particle size and long-term physical stability using High Pressure Homogenization technique. [ 4 ] Abdelbary et. al. (2009) , prepared SLNs of Diazepam (a poorly water-soluble drug ) by using high-shear homogenization and ultrasound techniques. This work also describes a new approach to prepare suppositories containing DZ-loaded SLN dispersions, as potential drug carrier for the rectal route. [5] Subedi et. al. (2009) , prepared Solid lipid nanoparticles (SLNs) of Doxorubicin by solvent emulsification diffusion method with Glyceryl caprate was used as lipid core, and curdlan as the shell material . [6]

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Alhaj et. al. (2008) , prepared SLNs of Tamoxifen by using hot high pressure homogenization techniques and concluded that Tamoxifen loaded SLNs display significant cytotoxicity against MCF-7 cells and may be considered as an alternative formulation for this anti-estrogen drug. [7 ] Esposito et. al. (2008) , concluded that nanostructured lipid carriers encapsulation may represent an effective strategy to prolong the half-life of bromocriptine . [8] Mandawgade et. al. (2008) , prepared solid lipid nanoparticles (SLNs) of lipophilic drug, Tretinoin (TRN) from indigenous natural solid (stearin fractions) lipids by using a simple microemulsion technique. [9]

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Zhang et. al. (2008) , prepared SLNs of adefovirdipivoxil (ADV) by solvent diffusion method, the inhibitory effects of ADV loaded in SLN on hepatitis B surface antigen, hepatitis B antigen and hepatitis B virus DNA levels in-vitro were significantly enhanced. [10 ] Lai et. al. (2007) , prepared two different SLN formulations of Artemisia arborescence essential oil with Compritol 888 ATO as lipid and Poloxamer 188 and Miranol Ultra C32 as surfactants by using the hot pressure homogenization technique . [11] Liu et. al. (2007) , prepared the various IT-SLN formulations by hot homogenization method for topical delivery of Isotretinoin. [12 ]

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Plian bang chang et. al. (2007) , prepared a cream containing Curcuminoids SLN by using microemulsion technique, and showed that application of cream was statistically significant in improving skin wrinkles, hydration, melanin content, biological elasticity, and viscoelasticity . [13] Pople et. al. (2006) , prepared the solid lipid nanoparticulate dispersion of vitamin A palmitate by using high-pressure homogenization technique and was incorporated into polymeric gels of Carbopol, Pemulen, Lutrol, and Xanthan gum for convenient topical application. [14 ] Maia et. al. (2000) , prepared the SLNs of prednicarbate (PC) and show the potential of SLNs as drug carriers for topical glucocorticoids. [15]

OBJECTIVE OF WORK: 

OBJECTIVE OF WORK

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The objective of the present study is to develop bioadhesive SLNs of Adapalene or SLNs of Adapalene incorporated into gel which would reduce the side effects of conventional formulation and enhance the penetration of drugs into the skin, increasing the treatment efficiency with sustained release action .

PLAN OF WORK: 

PLAN OF WORK

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1. PREFORMULATION STUDIES a ) Identification of drug Infrared spectroscopy UV/Visible spectroscopy b) Solubility analysis c) Partition coefficient d) Drug compatibility studies

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2. FORMULATION DEVELOPMENT a) Selection of material selection of lipid Selection of polymer b) Formulation technique Solvent emulsification-diffusion technique c) Optimization of drug-lipid ratio d) Optimization of processing parameters

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3. CHARACTERIZATION a) Characterization of SLNs i. Particle size and zeta potential ii. Entrapment efficiency EE = the amount of entrapped drug in SLN the amount of entrapped drug in SLN and free drug in dispersion. iii. In-vitro release study 4. STABILITY STUDIES The centrifuge test will be perform to assess the physical stability of the adapalene-loaded SLNs.

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METHODOLOGY

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SLNs can be prepared by any of the following methods:- a) High shear homogenization technique i . Hot homogenization ii . Cold homogenization b) Ultrasonication technique i . Probe Ultrasonication ii . Bath ultrasonication c) High pressure homogenization technique d) Solvent evaporation technique e) Microemulsion technique f) Spray drying

Methods of preparation: 

Methods of preparation Solid solution method Drug enriched shell method Drug enriched core method

REFERENCES: 

REFERENCES

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Vyas SP and Khar RK. Nanoparticles. In: Vyas SP and Khar RK, editors. Targeted and Controlled Drug Delivery - Novel Carrier Systems, New Delhi (India): CBS; 2002. p. 417-453 . Bhalekar MR, Pokharkar V, Madgulkar A and Patil N. Preparation and evaluation of miconazole nitrate loaded solid lipid nanoparticles for topical delivery. AAPS PharmSciTech 2009March 1; 10: 289-296 . Abdelbary G and Fahmy RH. Diazepam loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech 2009; 10: 211-218. Subedi RK, Kang KW, and Choi H. Preparation and characterization of solid lipid nanoparticles loaded with Doxorubicin. Eur J Pharm Sci 2009; 37: 508–513 .

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5) Alhaj NA, Abdullah R, Ibrahim S and Bustamam A. Tamoxifen drug loading solid lipid nanoparticles prepared by hot high pressure homogenization techniques. Am J PharmacolToxicol 2008; 3(3): 219-224. 6) Esposito E, Fantin M, Marti M, Drechsler M, Paccamiccio L, Mariani P, Sivieri E, Lain F, Menegatti E, Morari M, and Cortesi R. Solid Lipid Nanoparticles as Delivery Systems for Bromocriptine. Pharmaceutical Research 2008; 25: 1521-1530 . 7) Mandawgade SD, and Patravale VB. Development of SLNs from natural lipids: application to topical delivery of Tretinoin. Int J Pharm 2008; 363: 132–138.

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8) Zhang X, Miao J, Li M, Jiang S, Hu F, and Du Y. Solid lipid nanoparticles loading adefovirdipivoxil for antiviral therapy. J Zhejiang UniSci B 2008; 9(6): 506-510 . 9 ) Lai F, Sinico C, Logu AD, Zaru M, Müller RH, and Fadda AM. SLN as a topical delivery system for Artemisia arborescence essential oil: In vitro antiviral activity and skin permeation study. Int J Nanomed2007; 2(3): 419–425. 10 ) Liu J, Hu W, Chen H, Ni Q, Xu H, and Yang X. Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery. Int J Pharm 2007; 328: 191–195. 11) Plianbangchang P, Tungpradit W, and Tiyaboonchai W. Efficacy and safety of Curcuminoids loaded solid lipid nanoparticles facial cream as an anti-aging agent. Naresuan University Journal 2007; 15(2): 73-78 .

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12) Pople PV and Singh KK. Development and evaluation of topical formulation containing solid lipid nanoparticles of vitamin A. AAPSPharmSciTech 2006; 7(4): Article 91. 13) Maia CS, Mehnert W, and Korting MS. Solid lipid nanoparticles as drug carriers for topical glucocorticoids. Int J Pharm 2000; 196: 165–167.