Quercetin Solid Lipid Microparticle Stability and Deposition in Rat Lungs: A Study of Surfactant Effect
Article Sidebar
-
Inhalation, Solid Lipid Microparticle, Quercetin, Stability, Deposition, In vivo
Abstract
This study aims to determine the effect of surfactant concentration on Quercetin SLM as a potential carrier of respiratory diseases, especially ones resulting from oxidative stress injury. Quercetin is a natural antioxidant with high activity. SLM was formed with 5% compritol 888 ATO as a lipid and different concentrations of poloxamer 188 as a surfactant. SLM was produced by a combination of emulsification and sonication involving freeze drying. SLM is characterized by organolepsis, morphology, yield, particle size, drug loading, and entrapment efficiency. The antioxidant activity of quercetin SLMs was tested using the ABTS method. SLMs are characterized as having round and smooth morphology, high yield (F1 88.53%; F2 91.44%; F3 92.87%); particle size (F1 1.81 um; F2 1.90 um; F3 1.94 um); high drug loading (F1 15.96%; F2 13.74%; F3 13.19%); and high entrapment efficiency (F1 96.53%; F2 87.94%; F3 87.48%). Increasing surfactant concentration did not produce a significant difference between formulas. Quercetin SLM showed high antioxidant activity (Quercetin 94.43%; F1 94.35%; F2 94.36%; F3 94.37%). SLM was stable at storage temperatures between 25°C and 40°C. The effect of surfactant can be seen on particle size, drug loading, and entrapment efficiency at 40°C. Results of in vivo deposition study indicated that all SLM formulas were able to deliver quercetin to the lungs. Increasing the concentration of surfactant in Quercetin SLMs made no difference to the lung deposition as confirmed by observations conducted at 1 hour and 4 hours. Quercetin SLM has the potential for lung delivery by inhalation.
References
Ameya, D. M. M. (2017). Solid Lipid Nanoparticles in Drug Delivery: Opportunities and Challenges. In Emerging Nanotechnologies for Diagnostics, Drug Delivery, and Medical Devices. Elsavier, pages 291–330
Azizah, N., M. Rahmadi, and D. M. Hariyadi (2019). Effect of Sodium Alginate-Carrageenan Polymer Concentration on Drug Deposition of Ciprofloxacin Microspheres in Rat Lungs. Thesis, Airlangga University, Surabaya
Benke, E., A. Farkas, I. Balashazy, P. Szabo-Revesz, and R. Ambrus (2019). Stability Test of Novel Combined Formulated Dry Powder Inhalation System Containing Antibiotic: Physical Characterization and In Vitro–In Silico Lung Deposition Results. Drug Development and Industrial Pharmacy, 45(8); 1369–1378
Chen, W., S. Stolz, V. Wegbecher, D. Parakkattel, C. Haeuser, N. S. Oltra, R. S. K. Kishore, S. Bond, C. Bell, and R. Kopf (2022). The Degradation of Poloxamer 188 in Buffered Formulation Conditions. AAPS Open, 8; 5
Danaei, M., M. Dehghankhold, S. Ataei, F. H. Davarani, R. Javanmard, and A. Dokhani (2018). Impact of Particle Size and Polydispersity Index on the Clinical Applications of Lipidic Nanocarrier Systems. Pharmaceutics, 10(2); 57
Departemen Kesehatan Republik Indonesia (2020). Farmakope Indonesia Edisi VI. Departemen Kesehatan Republik Indonesia, Jakarta, Indonesia
Francesca, T., T. Camilla, Z. Yanxin, D. Giovanni, and D. Eros (2021). An Overview on Dietary Polyphenols and Their Biopharmaceutical Classification System (BCS). International Journal of Molecular Sciences, 22(11); 5514
Hariyadi, D. M., E. Hendradi, T. Erawati, E. N. Jannah, and W. Febrina (2018). Influence of Drug-Polymer Ratio on Physical Characteristics and Release of Metformin Hydrochloride from Metformin Alginate Microspheres. Tropical Journal of Pharmaceutical Research, 17(7); 1229–1233
Hariyadi, D. M., T. Purwanti, D. Maulydia, C. A. Estherline, E. Hendradi, and M. Rahmadi (2021). Performance and Drug Deposition of Kappa-Carrageenan Microspheres Encapsulating Ciprofloxacin HCl: Effect of Polymer Concentration. Journal of Advanced Pharmaceutical Technology and Research, 12; 242–249
Ignjatovic, J., J. Ðuriš, S. Cvijic, V. Dobricic, A. M. Lombardi, and S. Ibric (2021). Development of Solid Lipid Microparticles by Melt-Emulsification/Spray Drying Processes as Carriers for Pulmonary Drug Delivery. European Journal of Pharmaceutical Sciences, 156; 105588
Jung, H., Y. J. Lee, and W. B. Yoon (2018). Effect of Moisture Content on the Grinding Process and Powder Properties in Food: A Review. Processes, 6; 69
Kakran, M., R. Shegokar, N. G. Sahoo, S. Gohla, L. Li, and R. H. Müller (2012). Long-Term Stability of Quercetin Nanocrystals Prepared by Different Methods. Journal of Pharmacy and Pharmacology, 64; 1394–1402
Kaur, J., P. Muttil, R. K. Verma, K. Kumar, A. B. Yadav, R. Sharma, and A. Misra (2008). A Hand-Held Apparatus for "Nose-Only" Exposure of Mice to Inhalable Microparticles as a Dry Powder Inhalation Targeting Lung and Airway Macrophages. European Journal of Pharmaceutical Sciences, 34(4-5); 1–27
Kim, H., E. M. Seo, A. R. Sharma, B. Ganbold, J. Park, and G. Sharma (2013). Regulation of Wnt Signaling Activity for Growth Suppression Induced by Quercetin in 4T1 Murine Mammary Cancer Cells. International Journal of Oncology, 43; 1319–1325
Kumar, R., S. Vijayalakshmi, and S. Nadanasabapathi (2017). Health Benefits of Quercetin. Defence Life Science Journal, 2(2); 142–151
Mangal, S., R. Xu, H. Park, D. Zemlyanov, N. S. W. Lin, and D. Morton (2019). Understanding the Impacts of Surface Compositions on the In-Vitro Dissolution and Aerosolization of Co-Spray-Dried Composite Powder Formulations for Inhalation. Pharmaceutical Research, 36(6); 1–15
Mehta, P., C. Bothiraja, K. Mahadik, S. Kadam, and A. Pawar (2018). Phytoconstituent Based Dry Powder Inhalers as Biomedicine for the Management of Pulmonary Diseases. Biomedicine and Pharmacotherapy, 108; 828–837
Nahum, V. and A. J. Domb (2021). Recent Developments in Solid Lipid Microparticles for Food Ingredients Delivery. Foods, 10(2); 400
Patel, G. K., M. A. Khan, H. Zubair, S. K. Srivastava, M. Khushman, and S. Singh (2019). Comparative Analysis of Exosome Isolation Methods Using Culture Supernatant for Optimum Yield, Purity and Downstream Applications. Scientific Reports, 9; 5335
Queiros, M. D., R. L. Viriato, A. P. Ribeiro, and M. L. Gig ante (2020). Dairy-Based Solid Lipid Microparticles: A Novel Approach. Food Research International, 131; 109009
Rogers, L. K. and M. J. Cismowski (2018). Oxidative Stress in the Lung-The Essential Paradox. Current Opinion in Toxicology, 7; 37–43
Scalia, S., M. Haghi, V. Losi, V. Trotta, P. M. Young, and D. Traini (2013). Quercetin Solid Lipid Microparticles: A Flavonoid for Inhalation Lung Delivery. European Journal of Pharmaceutical Sciences, 49; 278–285
Scalia, S., P. M. Young, and D. Traini (2015). Solid Lipid Microparticles as an Approach to Drug Delivery. Expert Opinion on Drug Delivery, 12(4); 583–599
Shah, P. and H. Modi (2015). Comparative Study of DPPH, ABTS and FRAP Assays for Determination of Antioxidant Activity. International Journal for Research in Applied Science and Engineering Technology (IJRASET), 3(6); 636–641
Shetty, N., D. Cipolla, H. Park, and Q. T. Zhou (2020). Physical Stability of Dry Powder Inhaler Formulations. Expert Opinion on Drug Delivery, 17(1); 77–96
Sinko, P. J. (2016). Martin’s Physical Pharmacy and Pharmaceutical Sciences. Lippincott Williams & Wilkins, Baltimore & Philadelphia, 7th edition
Talarico, L., M. Consumi, G. Leone, and G. T. Magnani (2021). Solid Lipid Nanoparticles Produced via a Coacervation Method as Promising Carriers for Controlled Release of Quercetin. Molecules, 26; 2694
Wang, Y., P. Li, T. T. Tran, J. Zhang, and L. Kong (2016). Manufacturing Techniques and Surface Engineering of Polymer Based Nanoparticles for Targeted Drug Delivery to Cancer. Nanomaterials, 6(2); 26
Yang, D., T. Wang, M. Long, and P. Li (2020). Quercetin: Its Main Pharmacological Activity and Potential Application in Clinical Medicine. Oxidative Medicine and Cellular Longevity, 2020; 8825387
Authors
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.