Formulation and Evaluation of Solid Lipid Nanoparticles Loading Erythromycin Ethylsuccinate by Heating Emulsification and Homogenization Methods
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Keywords:
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Formulation, Lipid-Nanoparticles, Stearic-Acid, Erythromycin, Solubility
Abstract
The pandemic period has caused antibiotics highly recommended to cure infections. The use of macrolide antibiotics has greatly increased recently due to outbreaks of diseases that attack the human respiratory tract all of part of the world. One member of the macrolide group is erythromycin ethyl succinate which has low solubility in water. Therefore, this study aims to convert erythromycin ethyl succinate into lipid nanoparticles in an attempt to increase solubility. The method for the formation of nanoparticles is heating emulsification and homogenization. The results obtained in the form of formula 1 (F1) showed the percent encapsulation of 85.688±0.30641. The physical properties were that it has a size of 398.9±1.4 nm, a PDI of 0.3895±0.0015, and zeta potential of -17.45±0.15 mV respectively. The stability was determined by an accelerated test by the influence of extreme temperature and mechanics affecting the stability of the particles as an indication of decreasing the pH and particle precipitation. The solubility of erythromycin ethyl succinate in the form of lipid nanoparticles was increased in a comparison with the pure substance of erythromycin ethyl succinate.
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Watkins, R., L. Wu, C. Zhang, R. M. Davis, and B. Xu (2015). Natural Product-Based Nanomedicine: Recent Advances and Issues. International Journal of Nanomedicine, 10; 6055
Basu, S. and S. Smith (2021). Macrolides for The Prevention and Treatment of Feeding Intolerance in Preterm Low Birth Weight Infants: a Systematic Review and Meta-Analysis. European Journal of Pediatrics, 180(2); 353–378
Bhattacharyya, S. and P. Reddy (2019). Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles. Turkish Journal of Pharmaceutical Sciences, 16(4); 425
Blumenberg, V., M. L. Schubert, E. Zamir, S. Schmidt, R. Rohrbach, P. Waldhoff, D. Bozic, H. Pock, E. Elinav, and C. Schmidt (2020). Antibiotic Therapy and Low Gut Microbiome Diversity is Associated with Decreased Response and High Toxicity in BCP-ALL and DLBCL Patients after Treatment with CD19. CAR T-Cells. Blood, 136; 33–34
Cao, Y., S. Xuan, Y. Wu, and X. Yao (2019). Effects of Long-Term Macrolide Therapy at Low Doses in Stable COPD. International Journal of Chronic Obstructive Pulmonary Disease, 14; 1289
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 Crystallinity, 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
Fini, A., J. R. Moyano, J. M. Ginés, J. I. Perez-Martinez, and A. M. Rabasco (2005). Diclofenac Salts, II. Solid Dispersions in PEG6000 and Gelucire 50/13. European Journal of Pharmaceutics and Biopharmaceutics, 60(1); 99–111
Fonseca-Santos, B., P. B. Silva, R. B. Rigon, M. R. Sato, and M. Chorilli (2020). Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration. Current Medicinal Chemistry, 27(22); 3623-3656
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 Bioavailability of Glibenclamide. European Journal of Pharmaceutics and Biopharmaceutics, 102; 41–50
Gupta, B., B. K. Poudel, S. Pathak, J. W. Tak, H. H. Lee, J. H. Jeong, H. G. Choi, C. S. Yong, and J. O. Kim (2016). Effects of Formulation Variables on The Particle Size and Drug Encapsulation of Imatinib-Loaded Solid Lipid Nanoparticles. Aaps Pharmscitech, 17(3); 652–662
Ikeuchi-Takahashi, Y., C. Ishihara, and H. Onishi (2016). Formulation and Evaluation of Morin-Loaded Solid Lipid Nanoparticles. Biological and Pharmaceutical Bulletin, 39(9); b16–00300
Jain, G. and U. K. Patil (2015). Strategies for Enhancement of Bioavailability of Medicinal Agents with Natural Products. International Journal of Pharmaceutical Sciences and Research, 6(12); 5315–5324
Kalepu, S. and V. Nekkanti (2015). Insoluble Drug Delivery Strategies: Review of Recent Advances and Business Prospects. Acta Pharmaceutica Sinica B, 5(5); 442–453
Mahmood, H. S., M. Alaayedi, M. M. Ghareeb, and M. M. M. Ali (2020). The Enhancement Solubility of Oral Flurbiprofen by Using Nanoemelsion as Drug Delivery System. International Journal of Pharmaceutical Research, 12; 1612–1619
Mardiyanto, M., N. A. Fithri, A. Amriani, H. Herlina, and D. P. Sari (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
Martingano, D., S. Singh, and A. Mitrofanova (2020). Azithromycin in The Treatment of Preterm Prelabor Rupture of Membranes Demonstrates a Lower Risk of Chorioamnionitis and Postpartum Endometritis with an Equivalent Latency Period Compared with Erythromycin Antibiotic Regimens. Infectious Diseases in Obstetrics and Gynecology, 2020
Oliveira, M. S., S. V. Mussi, D. A. Gomes, M. I. Yoshida, F. Frezard, V. M. Carregal, and L. A. Ferreira (2016). ????-Tocopherol Succinate Improves Encapsulation and Anticancer Activity of Doxorubicin Loaded in Solid Lipid Nanoparticles. Colloids and Surfaces B: Biointerfaces, 140; 246–253
Pignatello, R., V. Fuochi, G. Petronio Petronio, A. S. Greco, and P. M. Furneri (2017). Formulation and Characterization of Erythromycin–Loaded Solid Lipid Nanoparticles. Biointerface Research in Applied Chemistry, 7(5); 32–39
Pignatello, R., A. Leonardi, V. Fuochi, G. Petronio Petronio, A. S. Greco, and P. M. Furneri (2018). A Method for Efficient Loading of Ciprofloxacin Hydrochloride in Cationic Solid Lipid Nanoparticles: Formulation and Microbiological Evaluation. Nanomaterials, 8(5); 304
Qiao, D., W. Shi, M. Luo, F. Jiang, and B. Zhang (2022). Polyvinyl Alcohol Inclusion Can Optimize The Sol-Gel, Mechanical and Hydrophobic Features of Agar/Konjac Glucomannan System. Carbohydrate Polymers, 277; 118879
Rapalli, V. K., S. Sharma, A. Roy, A. Alexander, and G. Singhvi (2021). Solid Lipid Nanocarriers Embedded Hydrogel for Topical Delivery of Apremilast: In-Vitro, Ex-Vivo, Dermatopharmacokinetic and Anti-Psoriatic Evaluation. Journal of Drug Delivery Science and Technology, 63; 102442
Rupenagunta, A., I. Somasundaram, V. Ravichandiram, J. Kausalya, and B. Senthilnathan (2011). Solid Lipid Nanoparticles-A Versatile Carrier System. Journal of Pharmaceutical Sciences, 4(7); 2069–2075
Sandi, S., F. Yosi, and M. L. Sari (2018). Preparation and Characterization of Bio-\ Polymeric Nano Feed Incorporating Silage-Derived Organic-Acids and The Polar Fraction of Papaya Leaf Extract. Journal of Physics: Conference Series, 1095; 012024
Sarathchandiran, I. (2012). A Review on Nanotechnology in Solid Lipid Nanoparticles. Journal of Pharmaceutical Development Technology, 2(1); 45–61
Surendra, B., M. N. Kumar, and P. Iriventi (2020). Formulation and Evaluation of Caffeine-Loaded Solid Lipid Nanoparticles to Treat Clinical Mastitis. Asian Journal of Pharmaceutical and Clinical Research, 23(3); 79–85
Untari, B., D. P. Wijaya, M. Mardiyanto, H. Herlina, and A. Firana (2019). Physical Interaction of Chitosan-Alginate Entrapping Extract of Papaya Leaf and Formation of Submicron Particles Dosage form: New Dossage form to Inhibit The Dengue Diseases. Science and Technology Indonesia, 4(3); 64–69
Watkins, R., L. Wu, C. Zhang, R. M. Davis, and B. Xu (2015). Natural Product-Based Nanomedicine: Recent Advances and Issues. International Journal of Nanomedicine, 10; 6055
Authors
Mardiyanto, M., Untari, B. ., Mara, A. ., Sinulingga, S. ., Syarif, N. ., & Ningsih, G. E. . (2022). Formulation and Evaluation of Solid Lipid Nanoparticles Loading Erythromycin Ethylsuccinate by Heating Emulsification and Homogenization Methods. Science and Technology Indonesia, 7(3), 320–326. https://doi.org/10.26554/sti.2022.7.3.320-326
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