DEVELOPMENT AND OPTIMIZATION OF POLYMERIC NANOPARTICLES OF GLYCYRRHIZIN: PHYSICOCHEMICAL CHARACTERIZATION AND ANTIOXIDANT ACTIVITY

DIVYA JYOTHI; SNEH PRIYA; JAINEY P. JAMES

doi:10.22159/ijap.2024v16i1.49164

Authors

DIVYA JYOTHI Department of Pharmacognosy, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences, Nitte (Deemed to be) University, Deralakatte, Karnataka, India https://orcid.org/0000-0002-8564-319X
SNEH PRIYA Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences, Nitte (Deemed to be) University, Deralakatte, Karnataka, India
JAINEY P. JAMES Department of Pharmaceutical Chemistry, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences, Nitte (Deemed to be) University, Deralakatte, Karnataka, India https://orcid.org/0000-0002-0564-8506

DOI:

https://doi.org/10.22159/ijap.2024v16i1.49164

Keywords:

Nanoparticles, Glycyrrhizin, Licorice

Abstract

Objective: The aim of the present study to develop, optimize and characterize Poly (D, L-lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) loaded with isolated Glycyrrhizin (Glyc) and investigate for antioxidant activity.

Methods: PLGA nanoparticles loaded with Glycyrrhizin were synthesized by an adapted emulsion-evaporation method. Nanoparticles were evaluated for particle size, entrapment efficiency and Polydispersiblity index (PDI). Further, Box Benkhen design was applied for optimization of the formulation parameters and the effect of three independent variables such as PLGA concentration, amount of glycyrrhizin, polyvinyl alcohol (PVA) concentration on particle size, polydispersiblity index and the entrapment efficiency (response variables) were investigated. The antioxidant capacity of optimized nanoparticle formulation loaded with glycyrrhizin was compared with free glycyrrhizin by DPPH assay.

Results: The particle size, entrapment efficiency and PDI of optimized Glyc-NPs was found to be 144.20 nm, 68.0% and 0.315 respectively. Optimized Glyc-NPs showed sustained release of drug 79.06% in 48 hours with improved free radical scavenging activity than isolated Glycyrrhizin.

Conclusion: PLGA nanoparticles were found to be suitable carrier for Glycyrrhizin at lower levels than originally required for enhanced functional properties.

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References

Krausse R, Bielenberg J, Blaschek W, Ullmann U. In vitro anti-helicobacter pylori activity of Extractum liquiritiae, glycyrrhizin and its metabolites. J. Antimicrob. Chemother. 2004;54:243–46

Huang RY, Chu YL, Jiang ZB, Chen XM, Zhang X, Zeng X. Glycyrrhizin suppresses lung adenocarcinoma cell growth through inhibition of thromboxane synthase. Cell. Physiol. Biochem. 2014; 33 (2):375–88

Roohbakhsh A, Iranshahy M, Iranshahi M. Glycyrrhetinic acid and its derivatives: anti-cancer and cancer chemo preventive properties, mechanisms of action and structure- cytotoxic activity relationship. Curr. Med. Chem. 2016;23 (5):498–517.

Duan E, Wang D, Fang L, Ma J, Luo J, Chen H, Li K, Xiao S,. Suppression of porcine reproductive and respiratory syndrome virus proliferation by glycyrrhizin. Antivir. Res.2015;120:122–25.

Imai K, Takagi Y, Iwazaki A, Nakanishi K. Radical scavenging ability of glycyrrhizin. Free radicals and antioxidants. 2013;3(1):40-2.

Wang W, Chen X, Zhang J, Zhao Y, Li S, Tan L, Gao J, Fang X, Luo A. Glycyrrhizin attenuates isoflurane-induced cognitive deficits in neonatal rats via its anti-inflammatory activity. Neuroscience. 2016 ;316:328-36.

Tu C, Li J, Wang F, Li L, Wang J, Jiang W. Glycyrrhizin regulates CD4 + T cell response during liver fibrogenesis via JNK, ERK and PI3K/AKT pathway. Int. Immunopharmacology. 2012;14 (4), 410–21.

Li X, Zhou A. Evaluation of the immunity activity of glycyrrhizin in AR mice. Molecules 2012;17:716–27.

Parisella ML, Angelone T, Gattuso A, Cerra MC, Pellegrino D. Glycyrrhizin and glycyrrhetinic acid directly modulate rat cardiac performance. The Journal of Nutritional Biochemistry. 2012 ;23(1):69-75.

Kumar S, Dilbaghi N, Saharan R, Bhanjana G. Nanotechnology as emerging tool for enhancing solubilty of poorly water-soluble drugs. Bio Nano Science 2012; 2(4):227-50

Jin S, Fu S, Han J, Jin S , Lv Q, Lu Y, Qi J, Wu W, Yuan H. Improvement of oral bioavailability of glycyrrhizin by sodium deoxycholate/phospholipid-mixed nano micelles, J. Drug Target. 2012;20(7):615-22

Wang Y, Qu W, Choi SH. FDA’s regulatory science program for generic PLA/PLGA-based drug products. American Pharmaceutical Review. 2016.

Stevanovic M, Uskokovic D. Poly (lactide-co-glycolide)-based micro and nanoparticles for the controlled drug delivery of vitamins. Current Nanoscience. 2009;5(1):1-4.

Xie X, Tao Q, Zou Y, Zhang F, Guo M, Wang Y, Wang H, Zhou Q, Yu S. PLGA nanoparticles improve the oral bioavailability of curcumin in rats: Characterizations and mechanisms. J Agric Food Chem. 2011 ;59(17):9280-9.

Mirazi, N., Shoaei, J., Khazaei, A., Hosseini, A., A comparative study on effect of metformin and metformin-conjugated nanotubes on blood glucose homeostasis in diabetic rats. Eur. J. Drug Metab. Pharmacokinet 2015; 40 (3), 343–48.

Kaushelendra M, Girendra KG. Isolation and characterization of glycyrrhetinic acid from root of glycyrrhiza glabra European J of Biomed and Pharm sciences. 2019;6(2): 528-33.

Mattu, C, Pabari, RM, Boffito M, Sartori S, Ciardelli G, Ramtoola Z. Comparative evaluation of novel biodegradable nanoparticles for the drug targeting to breast cancer cells. Eur. J. Pharm. Biopharm. 2013; 85:463–472.

Ferreira SL, Bruns RE, Ferreira HS, Matos GD, David JM, Brandao GC, Da Silva EG, Portugal LA, Dos Reis PS, Souza AS, Dos Santos WN. Box Behnken design: an alternative for the optimization of analytical methods. Anal. Chim. Acta 2007;597: 179–186.

Blois MS, Antioxidant determination using stable free radicals, Nature, 1958; 26:1199-1200.

Budhian A, Siegel SJ, Winey KI. Haloperidol-loaded PLGA nanoparticles: systematic study of particle size and drug content. International journal of pharmaceutics. 2007;336(2):367-75

Dubey N, Varshney R, Shukla J, Ganeshpurkar A, Hazari PP, Bandopadhaya GP, Mishra AK, Trivedi P. Synthesis, and evaluation of biodegradable PCL/PEG nanoparticles for neuroendocrine tumor targeted delivery of somatostatin analog. Drug delivery. 2012;19(3):132-42.

Sharma N, Madan P, Lin S. Effect of process and formulation variables on the preparation of parenteral paclitaxel-loaded biodegradable polymeric nanoparticles: A co-surfactant study. Asian journal of pharmaceutical sciences. 2016;11(3):404-16.

Tuba ST, Zerrin SB, Ulya B. Preparation of polymeric nanoparticles using different Stabilizing Agents. J. Fac. Pharm. Ankara 2009;38:257–268.

Talluri SV, Kuppusamy G, Karri VV, Yamjala K, Wadhwani A, Madhunapantula SV, Pindiprolu SS. Application of quality-by-design approach to optimize diallyl disulfide-loaded solid lipid nanoparticles. Artificial cells, nanomedicine, and biotechnology. 2017 ;45(3):474-88.

Panyam J, Williams D, Dash A, Leslie‐Pelecky D, Labhasetwar V. Solid‐state solubility influences encapsulation and release of hydrophobic drugs from PLGA/PLA nanoparticles. Journal of pharmaceutical sciences. 2004 ;93(7):1804-14.

Sharma D, Maheshwari D, Philip G, Rana R, Bhatia S, Singh M, Gabrani R, Sharma SK, Ali J, Sharma RK, Dang S. Formulation and optimization of polymeric nanoparticles for intranasal delivery of lorazepam using Box-Behnken design: in vitro and in vivo evaluation. BioMed research international. 2014; 11(3):404-416.

Shalaby KS, Soliman ME, Casettari L, Bonacucina G, Cespi M, Palmieri GF, Sammour OA, El Shamy AA. Determination of factors controlling the particle size and entrapment efficiency of noscapine in PEG/PLA nanoparticles using artificial neural networks. Int J. nanomed. 2014;9(1):4953-64.