Design and Optimization of PLGA-Based Tribulus terrestris Loaded Nanoparticles

Document Type : Original paper


1 Medicinal Plants Research Centre, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

2 Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

3 Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

4 Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

5 Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran


Background and Objectives: Novel drug delivery systems improve bioavailability of standardized plant extracts which enables them to cross the biological membranes. Biodegradable polymeric nanoparticle systems are an approach to circumvent problems in drug delivery. Tribulus terrestris growing in subtropical areas has exhibited some biological and pharmacological activities; it contains compounds like flavonoids and steroids. To improve bioavailability of active compounds of the plant, its extract was subjected to prepare nanoparticles. Methods: Aqueous ethanol 80% extract of the whole plant was used for preparation of encapsulated nanoparticles using poly DL-lactic-co-glycolic acid (PLGA) polymer. Mean particle size, polydispersity, drug loading and encapsulation efficiency of the nanoparticles systems were evaluated in various ratios of T. terrestris extract. Results: All the applied concentrations of the extract provided particles in nano-scale size (163-214 nm). By increasing the extract ratio encapsulation efficacy also increased ranging between 40.3-78.5%. Above 50% of the loaded extract released in the first 3 h and it continued for 10 days. Conclusion: the plant extract has been successfully encapsulated into PLGA polymer. The quantification of encapsulation efficiency and in vitro release also showed that application of the plant in pharmaceutical field can be improved using nanoparticles.


Main Subjects

[1] Snezhkina AV, Kudryavtseva AV, Kardymon OL, Savvateeva MV, Melnikova NV, Krasnov GS, Dmitriev AA. ROS generation and antioxidant defense systems in normal and malignant cells. Oxid Med Cell Longev. 2019; Article ID 6175804.
[2] Zhang J, Wang X, Vikash V, Ye Q, Wu D, Liu Y, Dong W. ROS and ROS mediated cellular signaling. Oxid Med Cell Longev. 2016; Article ID 4350965..
[3] Xu DP, Li Y, Meng X, Zhou T, Zhou Y, Zheng J, Zhang J-J, Li H-B. Natural antioxidants in foods and medicinal plants: extraction, assessment and resources. Int J Mol Sci. 2017; 18(1): 1–32.
[4] Zhang JJ, Li Y, Zhou T, Xu DP, Zhang P, Li S, Li HB. Bioactivities and health benefits of mushrooms mainly from China. Molecules. 2016; 21(7): 1–16.
[5] Li AN, Li S, Li HB, Xu DP, Xu XR, Chen F. Total phenolic contents and antioxidant capacities of 51 edible and wild flowers. J Funct Foods. 2014; 6: 319–330.
[6] Manayi A, Mirnezami T, Saeidnia S, Ajani Y. Pharmacognostical evaluation, phytochemical analysis and antioxidant activity of the roots of Achillea tenuifolia Lam. Pharmacogn J. 2012; 4(30): 14–19.
[7] Sarhadi E, Ebrahimi SN, Hadjiakhoondi A, Manayi A. Chemical composition and antioxidant activity of root essential oil of different Salvia leriifolia populations. J Essent Oil-Bear Plants. 2021; 24(10): 1–9.
[8] Apak R, Gorinstein S, Böhm V, Schaich KM, Özyürek M, Güçlü K. Methods of measurement and evaluation of natural antioxidant capacity/activity (IUPAC Technical Report). Pure Appl Chem. 2013; 85(5): 957–998.
[9] Grassi D, Desideri G, Ferri C. Flavonoids: antioxidants against atherosclerosis. Nutrients. 2010; 2(8): 889–902.
[10]Manayi A, Saeidnia S, Gohari AR, Abdollahi M. Methods for the discovery of new anti-aging products–targeted approaches. Expert Opin Drug Discov. 2014; 9(4): 383–405.
[11] Chhatre S, Nesari T, Somani G, Kanchan D, Sathaye S. Phytopharmacological overview of Tribulus terrestris. Pharmacogn Rev. 2014; 8(15): 45–51.
[12] Khare CP. Indian medicinal plants: an illustrated dictionary. New York: Springer Science & Business Media, 2008.
[13] Usman H, Abdulrahman F, Ladan A. Phytochemical and antimicrobial evaluation of Tribulus terrestris L. (Zygophylaceae). growing in Nigeria. Res J Bio Sci. 2007; 2(3): 244–247.
[14] Awasthi R, Kulkarni G, Pawar VK. Phytosomes: an approach to increase the bioavailability of plant extracts. Int J Pharm Pharm Sci. 2011; 3(2): 1–3.
[15] Wang S, Su R, Nie S, Sun M, Zhang J, Wu D, Moustaid-Moussa N. Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals. J Nutr Biochem. 2014; 25(4): 363–376.
[16] Paul S, Bhattacharyya SS, Boujedaini N, Khuda-Bukhsh AR. Anticancer potentials of root extract of Polygala senega and its PLGA nanoparticles-encapsulated form. Evid Based Complement Alternat Med. 2010; Article ID 517204.
[17] Ho ML, Fu YC, Wang GJ, Chen HT, Chang JK, Tsai TH, Wang CK. Controlled release carrier of BSA made by W/O/W emulsion method containing PLGA and hydroxyapatite. J Control Release. 2008; 128(2): 142–148.
[18] Esfandyari-Manesh M, Javanbakht M, Dinarvand R, Atyabi F. Molecularly imprinted nanoparticles prepared by miniemulsion polymerization as selective receptors and new carriers for the sustained release of carbamazepine. J Mater Sci Mater Med. 2012; 23(4): 963–972.
[19] Govender T, Stolnik S, Garnett MC, Illum L, Davis SS. PLGA nanoparticles prepared by nanoprecipitation: drug loading and release studies of a water soluble drug. J Control Release. 1999; 57(2): 171–185.
[20] Corrigan OI, Li X. Quantifying drug release from PLGA nanoparticulates. Eur J Pharm Sci. 2009; 37(3-4): 477–485.
[21] Eerikäinen H, Kauppinen EI. Preparation of polymeric nanoparticles containing corticosteroid by a novel aerosol flow reactor method. Int J Pharm. 2003; 263(1–2): 69–83.
[22] Mainardes RM, Gremião MPD, Evangelista RC. Thermoanalytical study of praziquantel-loaded PLGA nanoparticles. Rev Bras Cienc Farm. 2006; 42: 523–530.
[23] Joshi SA, Chavhan SS, Sawant KK. Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies. Eur J Pharm Biopharm. 2010; 76(2): 189–199.
[24] Pool H, Quintanar D, Figueroa JdD, Marinho Mano C, Bechara JEH, Godínez LA, Mendoza S. Antioxidant effects of quercetin and catechin encapsulated into PLGA nanoparticles. J Nanomater. 2012; Article ID 145380.
[25] Eloy JO, de Souza MC, Petrilli R, Barcellos JPA, Lee RJ, Marchetti JM. Liposomes as carriers of hydrophilic small molecule drugs: strategies to enhance encapsulation and delivery. Colloids Surf B Biointerfaces. 2014; 123: 345–363.
[26] Yamamoto T, Yokoyama M, Opanasopit P, Hayama A, Kawano K, Maitani Y. What are determining factors for stable drug incorporation into polymeric micelle carriers? Consideration on physical and chemical characters of the micelle inner core. J Control Release. 2007; 123(1): 11–18.