Solubility Enhancement of a Model Drug Quercetin by Nanotechnology Based Formulation Approach

Authors

  • Bashayer Alsofyani College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia
  • Reem Sari Alayli College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia
  • Maram Sari Alayli College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia
  • Teaf Salah Alkhaldi College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia
  • Ghadi Hammad Altalhi College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia
  • Mohammad Akhlaquer Rahman College of Pharmacy, Taif University, Haweiya, Taif-21974, Kingdom of Saudi Arabia https://orcid.org/0000-0003-1073-7279

DOI:

https://doi.org/10.55006/biolsciences.2023.3402

Keywords:

Solid lipid nanoparticles, Solubility, Quercetin, Encapsulation, Bioavailability, Stability

Abstract

Approximately, 40% of drug candidates have poor water solubility and its oral delivery is frequently associated with implications of low bioavailability, hepatic first-pass metabolism, enzymatic degradation, high intra- and inter subject variability, and lack of dose proportionality. Interests in solid lipid nanoparticles (SLN) to improve the oral bioavailability of such drugs (PWSD) are well known and documented in the literature. The aim of the research is to prepare solid lipid nanoparticles of quercetin by emulsification-ultrasonication method and evaluate the optimized formulation for solubility enhancement. Different batches of SLNs were prepared by emulsification-ultrasonication methods by changing process parameters, and finally on the basis of nanoparticle size, polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (EE), an optimum system was designed. The optimized formulation (Q-SLN9) demonstrated particle size, PDI, ZP, and EE; 327 nm, 0.118, 32.3 mV, and 57.9%, respectively. The optimized formulation has shown the highest zeta potential (-32.3 mV) confers its stability. In-vitro release of the drug showed significant improvement in the release of quercetin from SLN formulation as compared to plain drug. Furthermore, quercetin-loaded SLN was found to be stable at 4°C for 30 days of study period. The formulation was successfully prepared by the proposed method that can be used as a potential carrier for successful delivery of poorly water-soluble drugs associated with poor oral bioavailability.

Downloads

Download data is not yet available.

References

Klueglich M, Ring A, Scheuerer S, Trommeshauser D, Schuijt C, Liepold B, et al. Ibuprofen extrudate, a novel, rapidly dissolving ibuprofen formulation: relative bioavailability compared to ibuprofen lysinate and regular ibuprofen, and food effect on all formulations J. Clin. Pharmacol. 2005;42:1055-1061.

Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995;12:413-420.

Hiroshi A, Mikio T, Masahiro H. The novel formulation design of O/W microemulsion for improving the gastrointestinal absorption of poorly water-soluble compounds. Int. J. Pharm. 2005;305:61-74.

Sheikh S, Faiyaz S, Sushma T, Farhan JA, Roop RK, Mushir A. Development and bioavailability assessment of ramipril nanoemulsion formulation. Eur. J. Pharm. Sci. 2007;66:227-243.

Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self- emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm. Res. 1992;9:87-93.

Li P, Ghosh A, Wagner RF, Krill S, Joshi YM, Serajuddin ATM. Effect of combined use of nonionic surfactant on formation of oil-in-water microemulsions. Int. J. Pharm. 2005;288:27-34.

Kararli TT, Needham TE, Griffin M, Schoenhard G, Ferro LJ, Alcorn L. Oral delivery of a renin inhibitor compound using emulsion formulations. Pharm. Res. 1992;9:888-893.

Nakano M. Places of emulsions in drug delivery. Adv. Drug Deliv. Rev. 2000;45:1-4.

Schwendener RA, Schott H. Lipophilic 1-beta-D-arabinofuranosyl cytosine derivatives in liposomal formulations for oral and parenteral antileukemic therapy in the murine L1210 leukemia model. J. Cancer Res. Clin. Oncol. 1996;122:723-726.

Formica JV, Regelson W. Review of the biology of quercetin and related bioflavonoids. Food Chem Toxicol. 1995;33:1061-80.

Torchilin VP. “Micellar Nanocarriers: Pharmaceutical Perspectives”, Pharm Res. 2007;24(1):1-11.

Makris DP, Rossiter JT. 2000. Quercetin and rutin (quercetin 3-O- rhamnosylglucoside) thermal degradation in aqueous media under alkaline conditions. In: Buttriss J, Saltmarsh M, editors. Functional foods II: Claims and evidence. Cambridge, UK: Royal Society of Chemistry. pp 216–238.

Chen X, Zuo Z, Chow AHL, Chow MSS. 2001. Low bioavailability of quercetin in rats: Contributions by the gut and liver. AAPS PharmSci 3(S1). Abstract R5177. Available from: http://www. aapspharmsci.org/.

Manach C, Morand C, Crespy V, Demigne C, Taxier O, Regerat F, Remesy C. Quercetin is recovered in human plasma as conjugated derivatives which retain antioxidant properties. FEBS Lett. 1998;426:331-36.

Kim M, Sedykh A, Chakravarti SK, Saiakhov RD, Zhau H. Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches. Pharm Res. 2014;31(4):1002-1014.

Mehnert W, Mader K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2001;47(2):165-96.

Kakkar Thukral D, Dumoga S, Mishra AK. Solid lipid nanoparticles: promising therapeutic nanocarriers for drug delivery. Curr Drug Deliv. 2014;11(6):771-91

Q-y X, Wang M, Chen F, Gong T, Y-l J, Z-r Z. Lung-targeting delivery of dexamethasone acetate loaded solid lipid nanoparticles. Arch Pharm Res. 2007;30(4):519-25.

Muller RH, Keck CM. Challenges and solutions for the delivery of biotech drugs-a review of drug nanocrystal technology and lipid nanoparticles. J Biotechnol. 2004;113(1):151-70.

Mukherjee S, Ray S, Thakur R. Solid lipid nanoparticles: a modern formulation approach in drug delivery system. Indian J Pharm Sci. 2009;71(4):349.

Pardeike J, Hommoss A, Muller RH. Lipid nanoparticles (SLN/NLC) in cosmetic and pharmaceutical dermal products. Int J Pharm. 2009;366(1):170-84.

Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech. 2009;10(1):211 -9.

Kalepu S, Manthina M, Padavala V. Oral lipid-based drug delivery systems: An overview. Acta Pharm Sin B. 2013;3(6):361-72.

Aditya N, Macedo AS, Doktorovova S, Souto EB, Kim S, Chang P-S, et al. Development and evaluation of lipid nanocarriers for quercetin delivery: a comparative study of solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and lipid nanoemulsions (LNE). LWT-Food Sci Technol. 2014;59(1):115-21.

Joshi M, Patravale V. Formulation and evaluation of nanostructured lipid carrier (NLC)-based gel of valdecoxib. Drug Dev Ind Pharm. 2006;32:911-18.

Helgason T, Awad TS, Kristbergsson K, McClements DJ, Weiss J. Effect of surfactant surface coverage on formation of solid lipid nanoparticles (SLN). J Colloid Interface Sci. 2009;334:75-81.

Chen X, Zuo Z, Chow AHL, Chow MSS. 2001. Low bioavailability of quercetin in rats: Contributions by the gut and liver. AAPS PharmSci 3(S1).

Robhash KS, Keon WK, Hoo-Kyun C. Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin. Eur J Pharm Sci. 2009;37:508-13.

Pradhan M, Singh D, Singh MR. Influence of selected variables on fabrication of triamcinolone acetonide loaded solid lipid nanoparticles for topical treatment of dermal disorders. Artif Cells Nanomed Biotechnol. 2016;44(1): 392-400.

Eskandani M, Nazemiyeh H. Self-reporter shikonin-act-loaded solid lipid nanoparticle: Formulation, physicochemical characterization and geno/cytotoxicity evaluation. Eur J Pharm Sci. 2014;59:49.

Downloads

Published

22-11-2023
CITATION

How to Cite

Alsofyani, B., Sari Alayli, R., Sari Alayli, M., Salah Alkhaldi, T., Hammad Altalhi, G., & Akhlaquer Rahman, M. (2023). Solubility Enhancement of a Model Drug Quercetin by Nanotechnology Based Formulation Approach. Biological Sciences, 3(4), 509–515. https://doi.org/10.55006/biolsciences.2023.3402