Preparation of self-flocculated solid lipid nanoparticles
Yıl 2019,
Cilt: 23 Sayı: 4, 652 - 661, 27.06.2025
Ahmed Gardouh
El-sayed Khafagy
Mohamed Elkady
Öz
The objective of this study was to verify the effect of certain new biocompatible additive on the stability and feasibility of the SLN using Glyceryl monostearate as lipid matrix. Cationic Starch, which is newly modified in organic chemistry laboratories, used with different ratios to show the effect on zeta potential of formulated nanoparticles using Triamcinolone acetonide as a model drug. Method of High shear homogenization was used for preparation of SLN utilizing a rotor-stator homogenizer. It was found that particle diameter of formulated nanoparticles shifted from nanosized to micronized with increase of amount of cationic starch used (2.5 to 10% w/w), while the zeta potential reduced although showing high negative values (-36 to -27 mV), indicating stability. The loading capacity and encapsulation efficiency of produced nanoparticles were reduced with increase of amount of cationic starch used. The influence of cationic starch on drug release from prepared formulae was studied using dialysis bag technique. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drug and cationic starch. Electron microscope of scanning technique indicated sphere form of prepared solid lipid nanoparticles with smooth surface. It was concluded that retardation of in vitro release and effect on simulated in vivo permeation through human skin were affected by using different concentrations of cationic starch as excipient that meantime, be used to reduce zeta potential and act as self-flocculating agent during formulation.
Kaynakça
- [1] Pal S, Sen G, Carmaker NC, Mal D, Singh RP. High performance flocculating agents based on cationic polysaccharides in relation to coal fine suspension. Carbohyd Polym. 2008; 74(3): 590–596. [CrossRef]
- [2] Krentz D, Lohmann C, Schwarz S, et al. Properties and Flocculation Efficiency of Highly Cationized Starch Derivatives. Starch – Stärke. 2006; 58(3–4): 161–169. [CrossRef]
- [3] You L, Lu F, Li D, Qiao Z, Yin Y. Preparation and flocculation properties of cationic starch/chitosan crosslinking copolymer. J Hazard Mater. 2009; 172(1): 38–45. [CrossRef]
- [4] Jiang X, Qi Y, Wang S, Tian X. New amphoteric flocculant containing beta-cyclodextrin, synthesis, characterization and decolorization properties. J Hazard Mater. 2010; 173(1–3): 298–304. [CrossRef]
- [5] Chang Y, Choi H, Kim H, et al. Physicochemical properties of granular and non-granular cationic starches prepared under ultra-high pressure. Carbohyd Polym. 2014; 99: 385–393. [CrossRef]
- [6] Pal S, Mal D, Singh RP. Cationic starch: an effective flocculating agent. Carbohyd Polym. 2005; 59(4): 417–423. [CrossRef]
- [7] Wei Y, Cheng F, Zheng H. Synthesis and flocculating properties of cationic starch derivatives. Carbohyd Polym. 2008; 74(3): 673–679. [CrossRef]
- [8] Zhang B, Ni B, Lü S, et al. Synthesis and characterization of a novel potato starch derivative with cationic acetylcholine groups. Int J Biol Macromol. 2012; 50(3): 701–706. [CrossRef]
- [9] Pi-xin W, Xiu-li W, Xue D, et al. Preparation and characterization of cationic corn starch with a high degree of substitution in dioxane–THF–water media. Carbohyd Res. 2009; 344(7): 851–855. [CrossRef]
- [10] Raghavendra CM, Ramesh B, Vidhya R, et al. Nano/microTechnologies for Delivering Macromolecular Therapeutics using Poly (d, l-lactide-co-glycolide) and its Derivative. J Control Rel. 2008; 125: 193–209. [CrossRef]
- [11] 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: 161–177. [CrossRef]
- [12] Kavaliauskaite R, Klimaviciute R, Zemaitaitis A. Factors influencing production of cationic starches. Carbohyd Polym. 2008; 73(4–5): 665–675. [CrossRef]
- [13] Gardouh AR, Gad S, Ghonaim HM, Ghorab MM. Design and Characterization of Glyceryl Monostearate Solid Lipid Nanoparticles Prepared by High Shear Homogenization. Br J Pharm Res. 2013; 3(3): 326–346.
- [14] Mehnert W, Mader K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2001; 47: 165–196. [CrossRef]
- [15] Attama AA, Muller-Goymann CC. Effect of beeswax modification on the lipid matrix and solid lipid nanoparticle crystallinity. Coll Surf A Physicochem Eng Aspects. 2008; 315: 189–195. [CrossRef]
- [16] Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech. 2009; 10(1): 211–219. [CrossRef]
- [17] Bhalekar MR, Pokharkar V, Madgulkar A, et al. Preparation and evaluation of miconazole nitrate-loaded solid lipid nanoparticles for topical delivery. AAPS PharmSciTech. 2009; 10(1): 289–296. [CrossRef]
- [18] British Pharmacopoeia. Commission office. British Pharmacopoeia. The Stationery Office, London; 2009.
- [19] Feng W, Jian Y, Yu S, et al. Studies on PEG-modified SLNs loading vinorelbine bitartrate (I): Preparation and evaluation in vitro. Int J Pharm. 2008; 359: 104–110. [CrossRef]
- [20] Almeida AJ, Runge S, Muller RH. Peptide-loaded solid lipid nanoparticles (SLN): influence of production parameters. Int J Pharm. 1997; 149: 255–265. [CrossRef]
- [21] Lim S, Kim C. Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid. Int J Pharm. 2002; 243: 135–146. [CrossRef]
- [22] Harivardhan Reddy L, Murthy RS. Etoposide-loaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release, and stability evaluation. AAPS PharmSciTech. 2005; 6(2): E58–E166. [CrossRef]
- [23] Xiang L, Shu-fang N, Jun K, et al. A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers. Int J Pharm. 2008; 363: 177–182. [CrossRef]
- [24] 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. [CrossRef]
- [25] Ghorab MM, Abdel-Salam HM, Abdel-Moaty MM. Solid lipid nanoparticles – effect of lipid matrix and surfactant on their physical characteristics. Bull Pharm Sci, Assiut Univ. 2004; 27: 155–159.
- [26] Bisrat M, Anderberg EK, Barnett MI, Nyström C. Physicochemical aspects of drug release. XV. Investigation of diffusional transport in dissolution of suspended, sparingly soluble drugs. Int J Pharm. 1992; 80(1–3): 191–201. [CrossRef]
- [27] Pretsch E, Bühlmann P, Badertscher M. IR Spectroscopy. Structure Determination of Organic Compounds. Springer, Berlin Heidelberg; 2000: 267–320.
- [28] Da Silva-Junior AA, De Matos JR, Formariz TP, et al. Thermal behavior and stability of biodegradable spray-dried microparticles containing triamcinolone. Int J Pharm. 2009; 368: 45–55. [CrossRef]
- [29] Ansari M, Kazemipour M, Aklamli M. The study of drug permeation through natural membranes. Int J Pharm. 2006; 327: 6–11. [CrossRef]
- [30] Mei Z, Chen H, Weng T, et al. Solid lipid nanoparticles and microemulsion for topical delivery of triptolide. Eur J Pharm Biopharm. 2003; 56: 189–196. [CrossRef]
- [31] Jain SK, Chourasia MK, Masuriha R, et al. Solid lipid nanoparticles bearing flurbiprofen for transdermal delivery. Drug Deliv. 2005; 12: 207–215. [CrossRef]
- [32] Maia CS, Mehnert W, Schaller M, et al. Drug targeting by solid lipid nanoparticles for dermal use. J Drug Target. 2002; 10: 489–495. [CrossRef]
- [33] Chen H, Chang X, Du D, et al. Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting. J Control Rel. 2006; 110: 296–306. [CrossRef]
- [34] Lopes LB, Ferreira DA, Paula D, et al. Reverse hexagonal phase nano dispersion of monoolein and oleic acid for topical delivery of peptides: in vitro and in vivo skin penetration of cyclosporin A. Pharm Res. 2006; 23: 1332–1342. [CrossRef]
- [35] Liu J, Hu W, Chen H, et al. Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery
Yıl 2019,
Cilt: 23 Sayı: 4, 652 - 661, 27.06.2025
Ahmed Gardouh
El-sayed Khafagy
Mohamed Elkady
Kaynakça
- [1] Pal S, Sen G, Carmaker NC, Mal D, Singh RP. High performance flocculating agents based on cationic polysaccharides in relation to coal fine suspension. Carbohyd Polym. 2008; 74(3): 590–596. [CrossRef]
- [2] Krentz D, Lohmann C, Schwarz S, et al. Properties and Flocculation Efficiency of Highly Cationized Starch Derivatives. Starch – Stärke. 2006; 58(3–4): 161–169. [CrossRef]
- [3] You L, Lu F, Li D, Qiao Z, Yin Y. Preparation and flocculation properties of cationic starch/chitosan crosslinking copolymer. J Hazard Mater. 2009; 172(1): 38–45. [CrossRef]
- [4] Jiang X, Qi Y, Wang S, Tian X. New amphoteric flocculant containing beta-cyclodextrin, synthesis, characterization and decolorization properties. J Hazard Mater. 2010; 173(1–3): 298–304. [CrossRef]
- [5] Chang Y, Choi H, Kim H, et al. Physicochemical properties of granular and non-granular cationic starches prepared under ultra-high pressure. Carbohyd Polym. 2014; 99: 385–393. [CrossRef]
- [6] Pal S, Mal D, Singh RP. Cationic starch: an effective flocculating agent. Carbohyd Polym. 2005; 59(4): 417–423. [CrossRef]
- [7] Wei Y, Cheng F, Zheng H. Synthesis and flocculating properties of cationic starch derivatives. Carbohyd Polym. 2008; 74(3): 673–679. [CrossRef]
- [8] Zhang B, Ni B, Lü S, et al. Synthesis and characterization of a novel potato starch derivative with cationic acetylcholine groups. Int J Biol Macromol. 2012; 50(3): 701–706. [CrossRef]
- [9] Pi-xin W, Xiu-li W, Xue D, et al. Preparation and characterization of cationic corn starch with a high degree of substitution in dioxane–THF–water media. Carbohyd Res. 2009; 344(7): 851–855. [CrossRef]
- [10] Raghavendra CM, Ramesh B, Vidhya R, et al. Nano/microTechnologies for Delivering Macromolecular Therapeutics using Poly (d, l-lactide-co-glycolide) and its Derivative. J Control Rel. 2008; 125: 193–209. [CrossRef]
- [11] 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: 161–177. [CrossRef]
- [12] Kavaliauskaite R, Klimaviciute R, Zemaitaitis A. Factors influencing production of cationic starches. Carbohyd Polym. 2008; 73(4–5): 665–675. [CrossRef]
- [13] Gardouh AR, Gad S, Ghonaim HM, Ghorab MM. Design and Characterization of Glyceryl Monostearate Solid Lipid Nanoparticles Prepared by High Shear Homogenization. Br J Pharm Res. 2013; 3(3): 326–346.
- [14] Mehnert W, Mader K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2001; 47: 165–196. [CrossRef]
- [15] Attama AA, Muller-Goymann CC. Effect of beeswax modification on the lipid matrix and solid lipid nanoparticle crystallinity. Coll Surf A Physicochem Eng Aspects. 2008; 315: 189–195. [CrossRef]
- [16] Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech. 2009; 10(1): 211–219. [CrossRef]
- [17] Bhalekar MR, Pokharkar V, Madgulkar A, et al. Preparation and evaluation of miconazole nitrate-loaded solid lipid nanoparticles for topical delivery. AAPS PharmSciTech. 2009; 10(1): 289–296. [CrossRef]
- [18] British Pharmacopoeia. Commission office. British Pharmacopoeia. The Stationery Office, London; 2009.
- [19] Feng W, Jian Y, Yu S, et al. Studies on PEG-modified SLNs loading vinorelbine bitartrate (I): Preparation and evaluation in vitro. Int J Pharm. 2008; 359: 104–110. [CrossRef]
- [20] Almeida AJ, Runge S, Muller RH. Peptide-loaded solid lipid nanoparticles (SLN): influence of production parameters. Int J Pharm. 1997; 149: 255–265. [CrossRef]
- [21] Lim S, Kim C. Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid. Int J Pharm. 2002; 243: 135–146. [CrossRef]
- [22] Harivardhan Reddy L, Murthy RS. Etoposide-loaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release, and stability evaluation. AAPS PharmSciTech. 2005; 6(2): E58–E166. [CrossRef]
- [23] Xiang L, Shu-fang N, Jun K, et al. A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers. Int J Pharm. 2008; 363: 177–182. [CrossRef]
- [24] 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. [CrossRef]
- [25] Ghorab MM, Abdel-Salam HM, Abdel-Moaty MM. Solid lipid nanoparticles – effect of lipid matrix and surfactant on their physical characteristics. Bull Pharm Sci, Assiut Univ. 2004; 27: 155–159.
- [26] Bisrat M, Anderberg EK, Barnett MI, Nyström C. Physicochemical aspects of drug release. XV. Investigation of diffusional transport in dissolution of suspended, sparingly soluble drugs. Int J Pharm. 1992; 80(1–3): 191–201. [CrossRef]
- [27] Pretsch E, Bühlmann P, Badertscher M. IR Spectroscopy. Structure Determination of Organic Compounds. Springer, Berlin Heidelberg; 2000: 267–320.
- [28] Da Silva-Junior AA, De Matos JR, Formariz TP, et al. Thermal behavior and stability of biodegradable spray-dried microparticles containing triamcinolone. Int J Pharm. 2009; 368: 45–55. [CrossRef]
- [29] Ansari M, Kazemipour M, Aklamli M. The study of drug permeation through natural membranes. Int J Pharm. 2006; 327: 6–11. [CrossRef]
- [30] Mei Z, Chen H, Weng T, et al. Solid lipid nanoparticles and microemulsion for topical delivery of triptolide. Eur J Pharm Biopharm. 2003; 56: 189–196. [CrossRef]
- [31] Jain SK, Chourasia MK, Masuriha R, et al. Solid lipid nanoparticles bearing flurbiprofen for transdermal delivery. Drug Deliv. 2005; 12: 207–215. [CrossRef]
- [32] Maia CS, Mehnert W, Schaller M, et al. Drug targeting by solid lipid nanoparticles for dermal use. J Drug Target. 2002; 10: 489–495. [CrossRef]
- [33] Chen H, Chang X, Du D, et al. Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting. J Control Rel. 2006; 110: 296–306. [CrossRef]
- [34] Lopes LB, Ferreira DA, Paula D, et al. Reverse hexagonal phase nano dispersion of monoolein and oleic acid for topical delivery of peptides: in vitro and in vivo skin penetration of cyclosporin A. Pharm Res. 2006; 23: 1332–1342. [CrossRef]
- [35] Liu J, Hu W, Chen H, et al. Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery