EFFECT OF VISCOSITY, SURFACTANT TYPE AND CONCENTRATION ON PHYSICOCHEMICAL PROPERTIES OF SOLID LIPID NANOPARTICLES
Keywords:
Solid lipid nanoparticles, High shear homogenization, Tween 20, Tween 80, Glyceryl monostearate, Dibenzoyl peroxide, Erythromycin base, TriamcinoloneacetonideAbstract
Objective: The aim of the current work was to look into the feasibility of planning of solid lipid nanoparticles of Glyceryl mono stearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs.
Methods: Solid lipid nanoparticles loaded with three model lipophilic drugs were developed by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as the lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin asco-surfactant. Many formulation parameters were manipulated to receive high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standardphysical and imaging methods. The efficiency of drug release form prepared formulaewas studied using In vitro technique to utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectrum analysis.
The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and In vitro drug release behavior were too assessed.
Results: The average particle diameter measured by a laser diffraction technique was (194.6±5.03 to 406.6±15.2 NM) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) NM for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) NM for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultravioletspectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycinbase respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs(p˂0. 05). Thermal analysis of prepared solid lipid nanoparticles gave indication ofsolubilization of drugs within a lipid matrix. Fourier Transform Infrared Spectroscopy
(FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating nointeraction between drugs and lipid matrix and being only dissolved in it. Electronmicroscope of scanning and transmission techniques indicated sphere form of preparedsolid lipid nanoparticles with smooth surface with size below 100 nm.
Conclusion: In conclusion, it may be concluded that solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.
Â
Downloads
References
Kumaresh SS, Tejraj MA, Anandrao RK, Walter ER. Biodegradable polymeric nanoparticles as drug delivery devices. J Control Rel 2001;70(1-2):1-20.
Kiran C, Kuntal G, Mallikarjuna NN, Tejraj MA. Polymeric hydrogels for oral insulin delivery. J Control Rel 2013;165:129-38.
Schwarz C, Mehnert W, Lucks JS, Muller RH. Solid lipid nanoparticles (SLN) for controlled drug delivery. I. Production, characterization and sterilization. J Cont Rel 1994;30:83-96.
Raghavendra CM, Ramesh B, Vidhya R, Pradip P, Tejraj MA. Nano/micro technologies for delivering macromolecular therapeutics using poly (d, l-lactide-coglycolide) and its derivative. J Control Rel 2008;125:193-209.
Muller RH, Mader K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery-a review of the state of the art. Eur J Pharm Biopharm 2000;50:161-77.
Gupta AK, Lynde CW, Kunynetz RAW, Amin S, Choi KL, Goldstein E. A randomized, double-blind, multicenter, parallel group study to compare relative efficacies of the topical Gels 3% Erythromycin/5% Benzoyl Peroxide and 0.025 % tretinoin/ Erythromycin 4% in the Treatment of Moderate Acne Vulgaris of the Face. J Cuten Med Surg 2003;7(1):31-7.
Stecova J, Mehnert W, Blaschke T, Kleuser B, Sivaramakrishnan R, Zouboulis CC, et al. Cyproterone acetate loading to lipid nanoparticles for topical acne treatment: particle characterisation and skin uptake. Pharm Res 2007;24(5):991-1000.
Schafer-Korting M, Mehnert W, Korting HC. Lipid Nanoparticles for improved topical application of drugs for skin diseases. Adv Drug Deliv Rev 2007;59:427-43.
Yang YY, Wang Y, Powell R, Chan P. Polymeric core-shell Nanoparticles for therapeutics. Clin Exp Pharmacol Physiol 2006;33:557-62.
Mehnert W, Mader K. solid lipid Nanoparticles production, characterization and applications. Adv Drug Deliv Rev 2001;47;165-96.
British pharmacopoeia. Commission office. British pharmacopoeia. The stationaryoffice, London; 2009.
Amin AS, Issa YM. Selective spectrophotometric method for the determination oferythromycin and its esters in pharmaceutical formulations using gentian violet. J Pharm Biomed Anal 1996;14:1625-9.
Feng W, Jian Y, Yu S, Xing-Guo Z, Fu-De C, Yong-Zhong D, et al. Studies on PEG-modified SLNs loading vinorelbine bitartrate (I):Preparation andevaluation In vitro. Int J Pharm 2008;359:104-10.
Vivek K, Reddy H, Murthy RSR. Investigations of the effect of the lipid matrix on drug entrapment, In vitro release, and physical stability of olanzapine-loaded Solid Lipid Nanoparticles. AAPS Pharm Sci Tech 2007;8(4):83.
Le Verger ML, Fluckiger L, Kim Y, Hoffman M, Maincent P. Preparation andcharacterization of nanoparticles containing antihypertensive agent. Eur J Pharm Biopharm 1998;46:137-43.
Almeida AJ, Runge S, Muller RH. peptide–loaded solid lipid Nanoparticles (SLN): influence of production parameters. Int J Pharm 1997;149:255-65.
Bhalekar MR, Pokharkar V, Madgulkar A, Patil N. Preparation and evaluation of miconazole nitrate-loaded solid lipid nanoparticles for topical delivery. AAPS Pharm Sci Tech 2009;10(1):289-96.
Kim BD, Na K, Choi HK. Preparation and characterization of solid lipid Nanoparticles(SLN) made of cacao butter and curdlan. Eur J Pharm Sci 2005;24:199-205.
El-Laithy HM, Shoukry O, Mahran LG. Novel sugar esters proniosomes fortransdermal delivery of vinpocetine: Preclinical and clinical studies. Eur J Pharm Biopharm 2011;77(1):43-55.
Agnihotri SA, Mallikarjuna NN, Aminabhavi TM. Recent advances on chitosan-basedmicro-and nanoparticles in drug delivery. J Control Rel 2004;1:5-28.
Ghorab MM, Abdel-salam HM, Abdel-Moaty MM. Solid lipid Nanoparticles-effect oflipid matrix and surfactant on their physical characteristics. Bull Pharm Sci Assiut University 2004;27:155-9.
Bisrat M, Anderberg EK, Barnett MI, Nyström C. Physicochemical aspects of drugrelease. XV. Investigation of diffusional transport in dissolution of suspended, sparingly soluble drugs. Int J Pharm 1992;80(1-3):191-201.
Han F, Li S, Yin R, Liu H, Xu L. Effect of surfactants on the formation and characterization of a new type of colloidal drug delivery system: nanostructured lipidcarriers. Coll Surf A Physico Eng Aspec 2008;315:210–6.
Sznitowska M, Gajewska M, Janicki S, Radwanska A, Lukowski G. Bioavailability of DZ from aqueous-organic solution, submicron emulsion and solid lipid nanoparticlesafter rectal administration in rabbits. Eur J Pharm Biopharm 2001;52:159–63.
Muhlen A, Mehnert W. Drug release mechanism of prednisolone loaded solid lipidnanoparticles. Pharm 1998;53:552–5.
Muhlen A, Schwarz C, Mehnert W. Solid lipid nanoparticles (SLN) for controlled drugdelivery–drug release and release mechanism. Eur J Pharm Biopharm 1998;452:149–55.
Motwani SK, Chopra S, Talegaonkar S, Konchan K, Ahmed FJ, Khar RK. Chitosan –sodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: formulation, optimization and In vitro chacterization. Eur J Pharm Biopharm 2008;68:513-25.
Prabha FA, Zhou WZ, Panyam J, Labhasetwar V. Size dependency of nanoparticles mediated gene transfer: studies with fractionated nanoparticles. Int J Pharm 2002;244:105-15.
Pretsch E, Bühlmann P, Badertscher M. IR Spectroscopy, Structure determination of organic compounds. Springer Berlin Heidelberg 2000;267-320.
Pretsch E, Bühlmann P, Badertscher M. IR Spectroscopy. Structure determination of organic compounds. Springer Berlin Heidelberg 2009;1–67.
Sarisuta N, Kumpugdee M, Muller BW, Puttipipatkhachorn S. Physico-chemical characterization of interactions between erythromycin and various film polymers. Int J Pharm 1999;186:109-18.
Da Silva-Junior AA, De Matos JR, Formariz TP, Rossanezi G, Scarpa MV, Do Egito EST, et al. Thermal behavior and stability of biodegradable spray-driedmicroparticles containing triamcinolone. Int J Pharm 2009;368:45–55.
Freitas C, Müller RH. Correlation between long-term stability of solid lipidnanoparticles (SLN(TM)) and crystallinity of the lipid phase. Eur J Pharm Biopharm 1999;47:125–32.
Reddy LH, Murthy RS. Etoposide-loaded nanoparticles made from glyceride lipids: formulation, characterization, In vitro drug release, and stability evaluation. AAPS Pharm Sci Tech 2005;6(2):24.
Bunjes H, Westesen K, Koch MHJ. Crystallization tendency and polymorphictransitions in triglyceride nanoparticles. Int J Pharm 1996;129:159–73.
Araujo J, Mira-Gonzalez E, Egea MA, Garcia ML, Souto EB. Optimization and physicochemical characterization of a triamcinolone acetonide-loaded NLC for ocularantiangiogenic applications. Int J Pharm 2010;393;167-75.