Main Article Content
Ibuprofen (IBU) is a poorly water soluble non-steroidal anti-inflammatory drug with proven effectiveness for treating inflammatory, musculoskeletal, and rheumatic disorders. Nanocrystals (NCs) have been proposed as drug delivery systems to improve the solubility and bioavailability of poorly water-soluble compounds. Ibuprofen NCs (IBU-NCs) have been produced by melt-emulsification method using a combination of Tween®80/Span®80 as surfactant as these molecules are generally recognized as safe (GRAS) as non-toxic, non-irritating and are of low cost. The obtained main particle size (z-Ave) and polydispersity index (PdI) were 159.4 ± 3.265 nm and 0.24 ± 0.007, respectively. Lyophilization slightly increased the mean particle size and PdI compared to the non-freeze-dried IBU-NCs. The obtained IBU-NCs powders were of white and fine texture. The type and concentration of cryoprotector (trehalose, glucose, sucrose) influenced both the size and the in vitro release profile tested in Franz diffusion cells. Due to the smaller z-Ave, NCs:Trehalose (2:1) of 170.6 ± 3.880 nm (0.417 ± 0.050), NCs:Glucose (3:1) of 275.3 ± 8.351 nm (0.144 ± 0.021) and NCs:Sucrose (4:1) of 223.3 ± 10.35 nm (0.402 ± 0.016) were selected for the in vitro drug release tests. Within the first 6 hours, resuspended lyophilized nanocrystals released between 50-70% of the drug.
Papers may not be offered for publication elsewhere whilst under consideration by the International Journal of Advances in Medical Biotechnology - IJAMB. The corresponding author must obtain the consent of all co-authors to the submission of the paper. Papers accepted by the Journal for publication may not be published elsewhere without the permission of the JOURNAL and acknowledgement of the original source of the publication.
Jahnavi K, Reddy PP, Vasudha B, Narender B. Non-steroidal anti-inflammatory drugs: an overview. J Drug Deliv 2019;9(1-s):442-8.
Moilanen E, Vuolteenaho K. Nonsteroidal Anti-inflammatory Drugs. Nijkamp and Parnham's Principles of Immunopharmacology: Springer; 2019. p. 689-707.
Fernandes A, Dias-Ferreira J, Cabral C, Garcia M, Souto E. Release kinetics and cell viability of ibuprofen nanocrystals produced by melt-emulsification. Colloids and Surfaces B: Biointerfaces 1. 2018;166:24-8.
Fernandes A, Ferreira N, Fangueiro J, Santos A, Veiga F, Cabral C, et al. Ibuprofen nanocrystals developed by 22 factorial design experiment: a new approach for poorly water-soluble drugs. Saudi Pharm J 2017;25(8):1117-24.
Fernandes AR, Dias-Ferreira J, Ferreira-da-Silva C, Severino P, Martins-Gomes C, Silva AM, et al. Drug nanocrystals: Present, past and future. Applications of Nanocomposite Materials in Drug Delivery: Elsevier; 2018. p. 239-53.
Hofmann M, Thieringer F, Nguyen MA, Månsson W, Galle PR, Langguth P. A novel technique for intraduodenal administration of drug suspensions/solutions with concurrent pH monitoring applied to ibuprofen formulations. Eur J Pharm Biopharm. 2019;136:192-202.
Alves TFR, Barros CT, Baldo D, Amaral VA, Sever M, Santos C, et al. Preparation, Characterization and ex vivo Intestinal Permeability Studies of Ibuprofen Solid Dispersion. J Dispers Sci Technol. 2019;40(4):546-54.
Fangueiro JF, Marques IR, Severino P, Santana MHA, Souto EB. Desenvolvimento, produção e caracterização de nanocristais de fármacos pouco solúveis. Química Nova. 2012.
Fangueiro JF, Marques IR, Severino P, Santana MHA, Souto EB. Development, production and characterization of nanocrystals of poorly soluble drugs. Química Nova. 2012;35(9):1848-53.
Teeranachaideekul V, Junyaprasert VB, Souto EB, Muller RH. Development of ascorbyl palmitate nanocrystals applying the nanosuspension technology. Int J Pharm. 2008;354(1-2):227-34.
Muller RH, Runge S, Ravelli V, Mehnert W, Thunemann AF, Souto EB. Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals. Int J Pharm. 2006;317(1):82-9.
Cavendish M, Nalone L, Barbosa T, Barbosa R, Costa S, Nunes R, et al. Study of pre-formulation and development of solid lipid nanoparticles containing perillyl alcohol. JTAC. 2019:1-8.
Doktorovova S, Shegokar R, Fernandes L, Martins-Lopes P, Silva AM, Muller RH, et al. Trehalose is not a universal solution for solid lipid nanoparticles freeze-drying. Pharmaceutical development and technology. 2014;19(8):922-9.
Gol D, Thakkar S, Misra M. Nanocrystal-based drug delivery system of risperidone: lyophilization and characterization. Drug Dev Ind Pharm. 2018;44(9):1458-66.
Salim N, García-Celma MJ, Escribano E, Nolla J, Llinàs M, Basri M, et al. Formation of Nanoemulsion Containing Ibuprofen by PIC Method for Topical Delivery. Mater Today Proc. 2018;5:S172-S9.
Bagde A, Patel K, Kutlehria S, Chowdhury N, Singh M. Formulation of topical ibuprofen solid lipid nanoparticle (SLN) gel using hot melt extrusion technique (HME) and determining its anti-inflammatory strength. Drug Deliv Transl Res. 2019:1-12.
Alvarez-Román R, Naik A, Kalia Y, Guy RH, Fessi H. Skin penetration and distribution of polymeric nanoparticles. J Control Release. 2004;99(1):53-62.
Lademann J, Richter H, Meinke MC, Lange-Asschenfeldt B, Antoniou C, Mak WC, et al. Drug delivery with topically applied nanoparticles: science fiction or reality. Skin Pharmacol Physiol. 2013;26(4-6):227-33.
Adib ZM, Ghanbarzadeh S, Kouhsoltani M, Khosroshahi AY, Hamishehkar H. The effect of particle size on the deposition of solid lipid nanoparticles in different skin layers: A histological study. Adv Pharm Bull. 2016;6(1):31.
Nidhin M, Indumathy R, Sreeram K, Nair BU. Synthesis of iron oxide nanoparticles of narrow size distribution on polysaccharide templates. Bull Environ Contam Toxicol 2008;31(1):93-6.
Krause B, Mende M, Pötschke P, Petzold G. Dispersability and particle size distribution of CNTs in an aqueous surfactant dispersion as a function of ultrasonic treatment time. J Carbon. 2010;48(10):2746-54.
Sharma M, Mehta I. Surface stabilized atorvastatin nanocrystals with improved bioavailability, safety and antihyperlipidemic potential. Sci Rep. 2019;9(1):1-11.