Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles
DOI:
https://doi.org/10.37285/ijpsn.2010.3.3.12Abstract
Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h.
Downloads
Metrics
Keywords:
Solid lipid nanoparticles (SLNs), tripalmitin, polyvinyl alcohol, piroxicam, drug entrapment efficiencyDownloads
Published
How to Cite
Issue
Section
References
Almeida AJ, Runge S, Muller RH. Peptide-loaded solid lipid nanoparticles (SLN) influence of production parameters, Int. J. Pharm., 149, 255-265 (1997).
Alvarez-Figueroa MJ, Blanco-Mendeza J. Transdermal delivery of methotrexate: iontophoretic delivery from hydrogels and passive delivery from Microemulsion, Int. J. Pharm., 215, 57–65 (2001).
Bekerman T, Golenser J, Domb A. Ciclosporin nanoparticulate lipospheres for oral administration, J. Pharm. Sci. 93, 1264–1270 (2003).
Bocca C, Caputo O, Cavalli R, Gabriel L. Phagocytic uptake of fluorescent stealth and non-stealth solid lipid nanoparticles, Int. J. Pharm., 175, 185-193 (1998).
Borgia L S, Regehly M, Sivaramakrishnan R, Mehnert W, Korting HC, Danker K, Roder B, Kramer KD, Schfer-Korting M. Lipid nanoparticles for skin penetration enhancement correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy, J. Controlled Release, 110, 151– 163 (2005).
Casadei MA, Cerreto Cesa S, Feeney MGM, Marianecci C, Paolicell P. Solid lipid nanoparticles incorporated in dextran hydrogels: A new drug delivery system for oral formulation, Int. J. Pharm. (In Press) (2006).
Castelli F, Puglia C, Sarpietro MG, Rizza L, Bonina F. Characterization of indomethacin-loaded lipid nanoparticles by differential scanning calorimetry, Int. J. Pharm., 304, 231–238 (2005).
Cavalli R, Caputo O, Carlotti ME, Trotta M, Scarnecchia C, Gasco MR. Sterilization and freeze-drying of drug-free and drug-loaded solid lipid nanoparticles, Int. J. Pharm. 148, 47-54 (1997).
Cavalli R, Caputo O, Gasco MR. Preparation and characterization of solid lipid nanospheres containing Paclitaxel, Eur. J. Pharm. 10, 305–309 (2000).
Cavalli R, Peira E, Caputo O, Gasco MR. Solid lipid nanoparticles as carriers of hydrocortisone and progesterone complexes with beta-cyclodextrins, Int. J. Pharm., 182, 59–69 (1999).
Charcosset C, El-Harati A, Fessi H. Preparation of solid lipid nanoparticles using a membrane contactor, J. Controlled Release, 108,112– 120 (2005).
Chen H, Chang X, Du D, Liu W, Liu J, Weng T, Yang Y, Xu H, Yang X. Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting., J.Controlled Release, 110, 296 – 306 (2006).
Chen ZMH, Weng T, Yang Y, Yang X. Solid lipid nanoparticle and microemulsion for topical delivery of triptolide, Eur. J. Pharm. and Biopharm., 56,189–196 (2003).
Colombo AP, Briancon S, Lieto J, Fessi H. Project design and use of a pilot plant for nanocapsule production, Drug Dev. Ind. Pharm. 27, 1063–1072 (2001).
Cortesi R, Esposito E, Luca G, Nastruzzi, C. Production of lipospheres as carriers for bioactive compounds, Biomaterials 23, 2283–2294 (2002).
El-Ries MA. Spectrophotometric Determination of Piroxicam and Tenoxicam in Pharmaceutical Preparations Using Uranyl Acetate as a Chromogenic Agent., Analytical Letters, 31, 793 – 807 (2004).
Els-Shabouri MH. Positively charged nanoparticles for improving the oral bioavailability of cyclosporin-A, Int. J. Pharm., 249,101-108 (2002).
Florey K. Analytical profile of drug substances, Academic Press, Vol. 15, 509 (1979).
Freitas C, Muller RH. Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLNs) dispersions, Int. J. Pharm., 168, 221–229 (1998).
Fuentes MG, Prego C, Torres D, Alonso MJ. A comparative study of the potential of solid triglyceride nanostructures coated with chitosan or poly (ethylene glycol) as carriers for oral calcitonin delivery, Eur. J. Pharm. Sci. 25, 133–143 (2005).
Fuentes MG, Torres D, Alonso MJ. New surface-modified lipid nanoparticles as delivery vehicles for salmon calcitonin, Int. J. Pharm. 296, 122–132 (2005).
Garcia-Fuentes M, Torres D, Alonso MJ. Design of lipid nanoparticles for the oral delivery of hydrophilic macromolecules, Coll. Surf.B. Biointerfac., 27,159-168 (2002).
Gasco MR. Method for producing solid lipid microspheres having a narrow distribution, US Patent No. 5,250,236 (1993).
Goppert TG, Muller RM. Adsorption kinetics of plasma proteins on solid lipid nanoparticles for drug targeting, Int. J. Pharm. 302, 172–186 (2005).
Goppert TM, Muller RH. Protein adsorption patterns on poloxamer- and poloxamine-stabilized solid lipid nanoparticles (SLN), Eur. J.Pharm. and Biopharm., 60, 361–372 (2005).
Heiati H, Phillips NC, Tawashi R. Evidence for phospholipid bilayer formation in solid lipid nanoparticles formulated with phospholipid and triglyceride, Pharm. Research., Vol. 13, No.2 (1996).
Houa DZ, Xieb CS, Huangb K, Zhuc, CH. The production and characteristics of solid lipid nanoparticles (SLNs), Biomaterials, 24, 1781–1785 (2003).
Hu FQ, Jiang SP, Du YZ, Yuan H, Ye YQ, Zeng S. Preparation and characteristics of monostearin nanostructured lipid carriers, Int. J. Pharm., 314, 83–89 (2006).
Hu FQ, Jiang SP, Du YZ, Yuan H, Ye, YO, Zeng S. Preparation and characterization of stearic acid nanostructured lipidcarriers by solvent diffusion method in an aqueous system, Colld. Surf. B. Biointerfac, 45, 167–173 (2005).
Hu FQ, Yuan H, Zhang HH, Fang M. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization, Int. J. Pharm. 239, 121–128 (2002).
Indian Pharmacopeia, Govt. of India, Ministry of health and family welfare, Published by the controller of Publications, Delhi. Vol., I II, 1996.
Jee JP, Lim SJ, Park JS, Kim CK. Stabilization of all-trans retinol by loading lipophilic antioxidants in solid lipid nanoparticles, Eur. J.Pharm. and Biopharm.,63, 134–139 (2006).
Jie L, Wen Hu., Huabing Chena Qian N, Huibi Xu, Xiangliang Y. Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery, Int. J. Pharm., (2006).
Kenon AP, Schawartz M A. Drug stability, J. Am. Chem. Soc., 60, 2976-2981 (1983).
Kipp JK. The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs, Int. J. Pharm. 284, 109–122 (2004).
Kwon HY, Lee JH, Choi SW, Jang Y, Kim JH. Preparation of PLGA nanoparticles containing estrogen by emulsification diffusion method, Colloid Surf. A 182, 123–130 (2001).
Lachman L, Lieberman HA, Kanig LJ. The Theory and Practice of Industrial Pharmacy, Varghese Publishing House Bombay, 1987.
Lamprecht A, Saumet JL. Lipid nanocarriers as drug delivery system for ibuprofen in pain treatment, Int. J. Pharm. 278, 407–414 (2004).
Li Y, Dong L, Chang AJX, Xue H. Preparation and characterization of solid lipid nanoparticles loaded traditional chinese medicine, Int. J. Biological Macromolecules, 38, 296–299 (2006).
Lippacher A, Muller RH, Mader K. Semisolid SLNs dispersions for topical application: influence of formulation and production parameters on viscoelastic properties, Eur.J.Pharm.Biopharm., 53, 155–160 (2002).
Lippachera A, Muller RH, Mader K. Liquid and semisolid SLNe dispersions for topical application rheological characterization, Eur. J.Pharm. and Biopharm., 58, 561–567 (2004).
Maia CS, Mehnert W, Korting MHF. Solid lipid nanoparticles as drug carriers for topical glucocorticoids, Int. J. Pharm., 196, 165–167 (2000).
Marengo Emilio, Cavalli Roberta, Caputo Otto, Rodriguez Lorenzo, Gasco Maria Rosa. Scale-up of the preparation process of solid lipid nanospheres Part I, Int. J. Pharm., 205, 3–13 (2000).
Mehnert W, Mader K. Solid lipid nanoparticles Production, characterization and applications, Adv. Drug Del. Rev., 47, 165–196 (2001).
Meia Z, Lia X, Wua Q, Hua S, Yang X. The research on the anti-inflammatory activity and hepatotoxicity of triptolide-loaded solid lipid nanoparticles, Pharmacol. Res., 51, 345–351 (2005).
Miglietta A, Cavalli R, Bocca C, Gabriel L, Gasco MR. Cellular uptake and cytotoxicity of solid lipid nanospheres (SLN) incorporating doxorubicin or paclitaxel, Int. J. Pharm., 210, 61–67 (2000).
Morel S, Ugazio E, Cavalli R, Gasco MR. Thymopentin in solid lipid nanoparticles, Int. J. Pharm., 132, 259 261 (1996).
Morela S, Terrenob E, Ugazioa E, Aimeb S, Gascoa MR. NMR relaxometric investigations of solid lipi nanoparticles (SLN) containing gadolinium (III) complexes, Eur. J. Pharm. Biopharm., 45, 157–163 (1998).
Muller RH, Maeder K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery a review of the state of the art, Eur. J.Pharm. and Biopharm., 50,161-177 (2000).
Muller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations, Adv. Drug Deliv. Rev. 54 (1), S131–S155 (2002).
Muller RH, Rungea S, Ravelli V, Mehnert W, Thunemannc AF, Souto EB. Oral bioavailability of cyclosporine: Solid Lipid Nanoparticles (SLNs) versus drug nanocrystals, Int. J. Pharm. 317, 82–89 (2006).
Olbrich C, Gessner A, Kayser O, Muller RH. Lipid-drug conjugate (LDC) nanoparticles as novel carrier system for hydrophilic antitrypanosomal drug diminazenediaceturate, J. Drug Target. 10, 387–396 (2002).
Norouzi MR, Ganjali S, Labbafi A Mohammadi. Subsecond FFT-adsorptive Voltammetric Technique as a Novel Method for Subnano Level Monitoring of Piroxicam in its Tablets and Bulk Form at Au Microelectrode in Flowing Solutions, Analytical Letters, 40, 747-762 (2007).
Pandey R, Sharma S, Khuller GK. Tuberculosis: Oral solid lipid nanoparticle-based antitubercular chemotherapy, Tuberculosis. 85, 415–420 (2005).
Quintanar-Guerrero D, All´emann E, Doelker E, Fessi H. A mechanistic study of the formation of polymer nanoparticles by the emulsification-diffusion technique,Colloid. Polym. Sci. 275, 640–647 (1997).
Quintanar-Guerrero D, All´emann E, Fessi H., Doelker E. Preparation techniques and mechanisms of formation of biodegradable nanoparticles from preformed polymers, Drug Dev. Ind. Pharm. 24, 1113–1128 (1998a).
Quintanar-Guerrero D, Allemann E, Fessi H, Doelker E. Pseudolatex preparation using a novel emulsion-diffudion process involving direct displacement of partially water-miscible solvents by distillation, Int. J. Pharm. 188, 155–164 (1999b).
Quintanar-Guerrero D, Fessi H, Allemann E, Doelker E. Influence of stabilizing agents and preparative variables on the formation of poly (d,l-lactic acid) nanoparticles by an emulsification-diffusion technique, Int. J. Pharm. 143, 133–141 (1996).
Quintanar-Guerrero D, Ganem-Quintanar A, Allemann E, Fessi H, Doelker E. Influence of the stabilizer coating layer on the purification and freeze-drying of poly(d,l-lactic acid) nanoparticles prepared by an emulsion-diffusion technique, J. Microencapsul. 15, 107–119 (1998b).
Quintanar-Guerrero D, Gurny R, Allemann E, Fessi H, Doelker, E. Method for producing aqueous colloidal dispersions of nanoparticles. WO Patent No. 01,002,087 (1999a).
Reddy H, Murthy RSR. Etoposide-Loaded Nanoparticles Made from Glyceride Lipids: Formulation,Characterization, in Vitro Drug Release, and Stability Evaluation, AAPS, Pharm.Sci.Tech., 6(2), Article 24 (2005).
Saupe A, Gordon CK, Rades T. Structural investigations on nanoemulsions, solid lipid nanoparticles and nanostructured lipid carriers by cryo-field emission scanning electron microscopy and Raman spectroscopy, Int. J. Pharm., 314, 56–62 (2006).
Savaer AA, Karata Y, Ozkan N, Yüksel S A, Ozkan T Baykara. Validated LC Determination of the Piroxicam-ß-Cyclodextrin Inclusion Complex in Tablets and in Human Plasma, Chromatographia, 59, 555-560 (2004).
Schubert MA, Harms M, Muller-Goyman CC. Structural investigations on lipid nanoparticles containing high amounts of lecithin, Eur. J. pharm. Sci., 2 7, 226–236 (2006).
Schubert MA, Muller-Goymann CC. Characterisation of surface-modified solid lipid nanoparticles (SLN): Influence of lecithin and nonionic emulsifier, Eur. J.Pharm. and Biopharm., 61, 77–86 (2005).
Shahgaldian P, Da Silva E, Coleman AW, Rather B, Zaworoto MJ. Para-acyl-calyx-arene based solid lipid nanoparticles (SLNs) a detailed study of preparation and stability parameters, Int. J. Pharm. 253, 23–38 (2003).
Söderberg L, Dyhre H, Roth B, Bjorkman S. The “inverted cup” — A novel in vitro release technique for drugs in lipid formulations, J. Control. Release, 113, 80–88 (2006).
Souto, EB, Wissing SA, Barbosa CM, Muller RH. Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery, Int. J. Pharm., 278, 71–77 (2004).
Soutoa EB, Wissinga SA, Barbosab CM, Muller RH. Evaluation of the physical stability of SLN and NLC before and after incorporation into hydrogel formulations, Eur. J.Pharm. and Biopharm., 58, 83–90 (2004).
Tabatta K, Sametib M, Olbricha C, Muller RH, Lehrb CM. Effect of cationic lipid and matrix lipid composition on solid lipid nanoparticle-mediated gene transfer, Eur. J. Pharm. and Biopharm., 57,155–162 (2004).
The Merck Index. An Encyclopedia of Chemicals, Drug and Biologicals, 12th edition, Merch Research Laboratories, Division of Merck and Co., Inc., 7661, 1996.
Trotta M, Debernardi F, Caputo O. Preparation of solid lipid nanoparticles by a solvent emulsification–diffusion technique, Int. J. Pharm. 257, 153–160 (2003).
Venkateswarlu V, Manjunath K. Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles, J, Controlled Release, 95, 627–638 (2004).
Vyas SP, Khar RK, Controlled drug delivery concepts and advances, First edition, Vallabh Prakashan Delhi, (2002).
Westese, K, Bunjes H, Koch MHJ. Physicochemical characterization of lipid nanoparticles and evaluation of their loading capacity and sustained release potential, J, Controlled Release, 48, 223-236 (1997).
Westesen K, Siekmann B, Koch MHJ. Investigations on the physical state of lipid nanoparticles by synchroton radiation X-ray diffraction, Int. J. Pharm. 93, 189– 199 (1993).
Wissing SA, Kayser O, Muller RH. Solid lipid nanoparticles for parenteral drug delivery, Adv. Drug Deliv. Rev. 56, 1257–1272 (2004).
Yuan Y, Li S, Feng-kui Mo F, Zhong D. Investigation of microemulsion system for transdermaldelivery of meloxicam, Int. J. Pharm., (In Press) (2006).
Zhang N, Ping Q, Huang G, Xu W, Cheng Y, Han X. Lectin modified Solid Lipid Nanoparticles as Carriers for Oral Administration of Insulin, Int. J. Pharm., (In Press) (2006).
Zur Muhlen, A, Schwarz C, Mehnert W. Solid lipid nanoparticles (SLN) for controlled drug delivery- Drug release and release mechanism, Eur. J. Pharm. Biopharm, 45, 149-155 (1998).