Formulation and Characterization of Glibenclamide Solid Lipid Submicroparticles Formated by Virgin Coconut Oil and Solid Matrix Surfactant
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Keywords:
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glibenclamide, liquid-lipid, solid lipid nanoparticles, PEG-400
Abstract
Glibenclamide has the biopharmaceutics classification system (BCS) class II which has high permeability and low solubility. The solubility of glibenclamide can be enhanced by forming solid lipid nanoparticles (SLN). This research has the aim to prepare and characterize SLN loading glibenclamide. The glibenclamide SLN formula was composed by using the liquid lipid as virgin coconut oil (VCO), PEG 6000 as a solid matrix, tween 80 with various concentrations as a stabilizer, and PEG 400 as co-surfactant. Characterization was conducted by determining the encapsulation efficiency (%EE), size measurement, particle size distribution, and zeta potential of SLN glibenclamide. SLN formation was also tested for its physical stability based on the heating-cooling cycle method. The optimum formula was obtained at the concentration of tween-80 of 1 mg/mL yielding the %EE value of 60.6194%, and pH 6.01. The results of particles diameter analysis were 175.5 ± 10.07 nm with a polydispersity index (PDI) of 0.1270, and zeta potential of +5.9 mV respectively. Stability testing by the heating-cooling cycle method has shown the instability of the SLN glibenclamide form under extreme temperatures and mechanics. It could be concluded that the results of characterization of glibenclamide SLN showed appropriate physical properties for nanoparticulate formulation.
References
Ali, H. S. and A. F. Hanafy (2017). Glibenclamide nanocrystals in a biodegradable chitosan patch for transdermal delivery: engineering, formulation, and evaluation. Journal of pharma- ceutical sciences, 106(1); 402–410
Almanassra, I. W., E. C. Okonkwo, O. Alhassan, M. A. Atieh, V. Kochkodan, and T. Al-Ansari (2021). Stability and ther- mophysical properties test of carbide-derived carbon ther- mal fluid; a comparison between functionalized and emulsi- fied suspensions. Powder Technology, 377; 415–428
Amin, O., D. Cartwright, and M. Azharuddin (2020). 1 Hyper- glycaemia in T1DM and pancreatitis related diabetes. The Fellowship of Postgraduate Medicine, 96; 119
Boukhors, Y., R. Rabasa-Lhoret, H. Langelier, M. Soultan, A. Lacroix, and J. Chiasson (2003). The use of information technology for the management of intensive insulin therapy in type 1 diabetes mellitus. Diabetes & metabolism, 29(6); 619–627
Chantaburanan, T., V. Teeranachaideekul, D. Chantasart, A. Jintapattanakit, and V. B. Junyaprasert (2017). Effect of binary solid lipid matrix of wax and triglyceride on lipid crys- tallinity, drug-lipid interaction and drug release of ibuprofen- loaded solid lipid nanoparticles (SLN) for dermal delivery. Journal of colloid and interface science, 504; 247–256
Colmers, I., S. Bowker, L. Tjosvold, and J. Johnson (2012). Insulin use and cancer risk in patients with type 2 diabetes: a systematic review and meta-analysis of observational studies. Diabetes & metabolism, 38(6); 485–506
das Neves, J., M. Amiji, M. F. Bahia, and B. Sarmento (2013). Assessing the physical–chemical properties and stability of dapivirine-loaded polymeric nanoparticles. International journal of pharmaceutics, 456(2); 307–314
Diwan, V., G. Gobe, and L. Brown (2014). Glibenclamide improves kidney and heart structure and function in the adenine-diet model of chronic kidney disease. Pharmacologi- cal Research, 79; 104–110
Fini, A., J. R. Moyano, J. M. Ginés, J. I. Perez-Martinez, and A. M. Rabasco (2005). Diclofenac salts, II. Solid disper- sions in PEG6000 and Gelucire 50/13. European journal of pharmaceutics and biopharmaceutics, 60(1); 99–111
Freitas, C. and R. Müller (1999). Correlation between long- term stability of solid lipid nanoparticles (SLNTM) and crys- tallinity of the lipid phase. European journal of pharmaceutics and biopharmaceutics, 47(2); 125–132
Fu, D., P. Zhang, L. Du, and J. Dai (2014). Experiment and model for the viscosities of MEA-PEG400, DEA-PEG400 and MDEA-PEG400 aqueous solutions. The Journal of Chem- ical Thermodynamics, 78; 109–113
Geng, T., C. Zhang, Y. Jiang, H. Ju, and Y. Wang (2017). Syn- ergistic effect of binary mixtures contained newly cationic surfactant: Interaction, aggregation behaviors and applica- tion properties. Journal of Molecular Liquids, 232; 36–44
Gonçalves, L., F. Maestrelli, L. D. C. Mannelli, C. Ghelardini, A. Almeida, and P. Mura (2016). Development of solid lipid nanoparticles as carriers for improving oral bioavail- ability of glibenclamide. European Journal of Pharmaceutics and Biopharmaceutics, 102; 41–50
Hanafy, A., H. Spahn-Langguth, G. Vergnault, P. Grenier, M. T. Grozdanis, T. Lenhardt, and P. Langguth (2007). Pharmacokinetic evaluation of oral fenofibrate nanosuspen- sions and SLN in comparison to conventional suspensions of micronized drug. Advanced drug delivery reviews, 59(6); 419–426
Hardoon, D. R., S. Szedmak, and J. Shawe-Taylor (2004). Canonical correlation analysis: An overview with application to learning methods. Neural computation, 16(12); 2639–2664 Jensen, L. B., E. Magnussson, L. Gunnarsson, C. Vermehren, H. M. Nielsen, and K. Petersson (2010). Corticosteroid
solubility and lipid polarity control release from solid lipid nanoparticles. International journal of pharmaceutics, 390(1); 53–60
Khan, S., A. Madni, M. A. Rahim, H. Shah, A. Jabar, M. M. Khan, A. Khan, N. Jan, and M. A. Mahmood (2021). Enhanced in vitro release and Permeability of Gliben- clamide by Proliposomes: Development, Characterization and Histopathological Evaluation. Journal of Drug Delivery Science and Technology, 63; 102450
Li, D., X. Wu, X. Yu, Q. Huang, and L. Tao (2015). Synergistic effect of non-ionic surfactants Tween 80 and PEG6000 on cytotoxicity of insecticides. Environmental toxicology and pharmacology, 39(2); 677–682
Lindenberg, M., S. Kopp, and J. B. Dressman (2004). Classi- fication of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. European Journal of Pharmaceutics and Biopharmaceutics, 58(2); 265–278
Maretti, E., B. Pavan, C. Rustichelli, M. Montanari, A. Dalpiaz, V. Iannuccelli, and E. Leo (2021). Chitosan/heparin poly- electrolyte complexes as ion-paring approach to encapsulate heparin in orally administrable SLN: In vitro evaluation. Col- loids and Surfaces A: Physicochemical and Engineering Aspects, 608; 125606
Maritim, S., P. Boulas, and Y. Lin (2021). Comprehensive analysis of liposome formulation parameters and their influ- ence on encapsulation, stability and drug release in gliben- clamide liposomes. International Journal of Pharmaceutics, 592; 120051
Price, D. J., A. Nair, J. Becker-Baldus, C. Glaubitz, M. Kuentz, J. Dressman, and C. Saal (2020). Incorporation of HPM-
CAS during loading of glibenclamide onto mesoporous silica improves dissolution and inhibits precipitation. European Journal of Pharmaceutical Sciences, 141; 105113
Rupenagunta, A., I. Somasundaram, V. Ravichandiram, J. Kausalya, and B. Senthilnathan (2011). Solid lipid nanoparticles-A versatile carrier system. Journal of Pharmacy Research, 4(7); 2069–2075
Sarathchandiran, I. (2012). A review on nanotechnology in solid lipid nanoparticles. International Journal of Pharmaceuti- cal Development and Technology, 2(1); 45–61
Senior, P. A., R. L. Houlden, J. Kim, D. Mackay, S. Nagpal, D. Rabi, D. Sherifali, and H. S. Bajaj (2020). Pharmaco- logic Glycemic Management of Type 2 Diabetes in Adults: 2020 Update–The User’s Guide. Canadian Journal of Diabetes, 44(7); 592–596
Shakeel, F., N. Haq, F. Alanazi, and I. Alsarra (2014). Effect of oils and surfactants on physicochemical characterization and in vitro dissolution of glibenclamide from self-emulsifying formulations. Journal of Drug Delivery Science and Technology, 24(1); 78–85
Tekin, Z. H., E. Avci, S. Karasu, and O. S. Toker (2020). Rapid determination of emulsion stability by rheology-based
thermal loop test. LWT- Food Science and Technology, 122; 109037
Yazar, A., G. Polat, I. Ün, A. Levent, A. Kaygusuz,K. Büyükafşar, et al. (2002). Effects of glibenclamide, met- formin and insulin on the incidence and latency of death by oubain-induced arrhythmias in mice. Pharmacological research, 45(3); 183–187
Yokoyama, A., K. R. Srinivasan, and H. S. Fogler (1988). Sta- bilization mechanism of colloidal suspensions by gum traga- canth: the influence of pH on stability. Journal of Colloid and Interface Science, 126(1); 141–149
Almanassra, I. W., E. C. Okonkwo, O. Alhassan, M. A. Atieh, V. Kochkodan, and T. Al-Ansari (2021). Stability and ther- mophysical properties test of carbide-derived carbon ther- mal fluid; a comparison between functionalized and emulsi- fied suspensions. Powder Technology, 377; 415–428
Amin, O., D. Cartwright, and M. Azharuddin (2020). 1 Hyper- glycaemia in T1DM and pancreatitis related diabetes. The Fellowship of Postgraduate Medicine, 96; 119
Boukhors, Y., R. Rabasa-Lhoret, H. Langelier, M. Soultan, A. Lacroix, and J. Chiasson (2003). The use of information technology for the management of intensive insulin therapy in type 1 diabetes mellitus. Diabetes & metabolism, 29(6); 619–627
Chantaburanan, T., V. Teeranachaideekul, D. Chantasart, A. Jintapattanakit, and V. B. Junyaprasert (2017). Effect of binary solid lipid matrix of wax and triglyceride on lipid crys- tallinity, drug-lipid interaction and drug release of ibuprofen- loaded solid lipid nanoparticles (SLN) for dermal delivery. Journal of colloid and interface science, 504; 247–256
Colmers, I., S. Bowker, L. Tjosvold, and J. Johnson (2012). Insulin use and cancer risk in patients with type 2 diabetes: a systematic review and meta-analysis of observational studies. Diabetes & metabolism, 38(6); 485–506
das Neves, J., M. Amiji, M. F. Bahia, and B. Sarmento (2013). Assessing the physical–chemical properties and stability of dapivirine-loaded polymeric nanoparticles. International journal of pharmaceutics, 456(2); 307–314
Diwan, V., G. Gobe, and L. Brown (2014). Glibenclamide improves kidney and heart structure and function in the adenine-diet model of chronic kidney disease. Pharmacologi- cal Research, 79; 104–110
Fini, A., J. R. Moyano, J. M. Ginés, J. I. Perez-Martinez, and A. M. Rabasco (2005). Diclofenac salts, II. Solid disper- sions in PEG6000 and Gelucire 50/13. European journal of pharmaceutics and biopharmaceutics, 60(1); 99–111
Freitas, C. and R. Müller (1999). Correlation between long- term stability of solid lipid nanoparticles (SLNTM) and crys- tallinity of the lipid phase. European journal of pharmaceutics and biopharmaceutics, 47(2); 125–132
Fu, D., P. Zhang, L. Du, and J. Dai (2014). Experiment and model for the viscosities of MEA-PEG400, DEA-PEG400 and MDEA-PEG400 aqueous solutions. The Journal of Chem- ical Thermodynamics, 78; 109–113
Geng, T., C. Zhang, Y. Jiang, H. Ju, and Y. Wang (2017). Syn- ergistic effect of binary mixtures contained newly cationic surfactant: Interaction, aggregation behaviors and applica- tion properties. Journal of Molecular Liquids, 232; 36–44
Gonçalves, L., F. Maestrelli, L. D. C. Mannelli, C. Ghelardini, A. Almeida, and P. Mura (2016). Development of solid lipid nanoparticles as carriers for improving oral bioavail- ability of glibenclamide. European Journal of Pharmaceutics and Biopharmaceutics, 102; 41–50
Hanafy, A., H. Spahn-Langguth, G. Vergnault, P. Grenier, M. T. Grozdanis, T. Lenhardt, and P. Langguth (2007). Pharmacokinetic evaluation of oral fenofibrate nanosuspen- sions and SLN in comparison to conventional suspensions of micronized drug. Advanced drug delivery reviews, 59(6); 419–426
Hardoon, D. R., S. Szedmak, and J. Shawe-Taylor (2004). Canonical correlation analysis: An overview with application to learning methods. Neural computation, 16(12); 2639–2664 Jensen, L. B., E. Magnussson, L. Gunnarsson, C. Vermehren, H. M. Nielsen, and K. Petersson (2010). Corticosteroid
solubility and lipid polarity control release from solid lipid nanoparticles. International journal of pharmaceutics, 390(1); 53–60
Khan, S., A. Madni, M. A. Rahim, H. Shah, A. Jabar, M. M. Khan, A. Khan, N. Jan, and M. A. Mahmood (2021). Enhanced in vitro release and Permeability of Gliben- clamide by Proliposomes: Development, Characterization and Histopathological Evaluation. Journal of Drug Delivery Science and Technology, 63; 102450
Li, D., X. Wu, X. Yu, Q. Huang, and L. Tao (2015). Synergistic effect of non-ionic surfactants Tween 80 and PEG6000 on cytotoxicity of insecticides. Environmental toxicology and pharmacology, 39(2); 677–682
Lindenberg, M., S. Kopp, and J. B. Dressman (2004). Classi- fication of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. European Journal of Pharmaceutics and Biopharmaceutics, 58(2); 265–278
Maretti, E., B. Pavan, C. Rustichelli, M. Montanari, A. Dalpiaz, V. Iannuccelli, and E. Leo (2021). Chitosan/heparin poly- electrolyte complexes as ion-paring approach to encapsulate heparin in orally administrable SLN: In vitro evaluation. Col- loids and Surfaces A: Physicochemical and Engineering Aspects, 608; 125606
Maritim, S., P. Boulas, and Y. Lin (2021). Comprehensive analysis of liposome formulation parameters and their influ- ence on encapsulation, stability and drug release in gliben- clamide liposomes. International Journal of Pharmaceutics, 592; 120051
Price, D. J., A. Nair, J. Becker-Baldus, C. Glaubitz, M. Kuentz, J. Dressman, and C. Saal (2020). Incorporation of HPM-
CAS during loading of glibenclamide onto mesoporous silica improves dissolution and inhibits precipitation. European Journal of Pharmaceutical Sciences, 141; 105113
Rupenagunta, A., I. Somasundaram, V. Ravichandiram, J. Kausalya, and B. Senthilnathan (2011). Solid lipid nanoparticles-A versatile carrier system. Journal of Pharmacy Research, 4(7); 2069–2075
Sarathchandiran, I. (2012). A review on nanotechnology in solid lipid nanoparticles. International Journal of Pharmaceuti- cal Development and Technology, 2(1); 45–61
Senior, P. A., R. L. Houlden, J. Kim, D. Mackay, S. Nagpal, D. Rabi, D. Sherifali, and H. S. Bajaj (2020). Pharmaco- logic Glycemic Management of Type 2 Diabetes in Adults: 2020 Update–The User’s Guide. Canadian Journal of Diabetes, 44(7); 592–596
Shakeel, F., N. Haq, F. Alanazi, and I. Alsarra (2014). Effect of oils and surfactants on physicochemical characterization and in vitro dissolution of glibenclamide from self-emulsifying formulations. Journal of Drug Delivery Science and Technology, 24(1); 78–85
Tekin, Z. H., E. Avci, S. Karasu, and O. S. Toker (2020). Rapid determination of emulsion stability by rheology-based
thermal loop test. LWT- Food Science and Technology, 122; 109037
Yazar, A., G. Polat, I. Ün, A. Levent, A. Kaygusuz,K. Büyükafşar, et al. (2002). Effects of glibenclamide, met- formin and insulin on the incidence and latency of death by oubain-induced arrhythmias in mice. Pharmacological research, 45(3); 183–187
Yokoyama, A., K. R. Srinivasan, and H. S. Fogler (1988). Sta- bilization mechanism of colloidal suspensions by gum traga- canth: the influence of pH on stability. Journal of Colloid and Interface Science, 126(1); 141–149
Authors
Mardiyanto, M., Fithri, N. A., Amriani, A., Herlina, H., & Sari, D. P. (2021). Formulation and Characterization of Glibenclamide Solid Lipid Submicroparticles Formated by Virgin Coconut Oil and Solid Matrix Surfactant. Science and Technology Indonesia, 6(2), 58–66. https://doi.org/10.26554/sti.2021.6.2.58-66
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