FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES

Authors

  • Y. SARAH SUJITHA Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam, (Women’s University), Tirupati, India
  • Y. INDIRA MUZIB Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam, (Women’s University), Tirupati, India

DOI:

https://doi.org/10.22159/ijap.2019v11i5.32850

Keywords:

Nanosponges, Nanosponges gel, Quercetin, In vitro, Ex-vivo studies, In vivo studies

Abstract

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug.

Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies.

Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation.

Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

Downloads

Download data is not yet available.

References

Soo Nam Park, Hye Jin Lee, Hae Soo Kim, Min A Park, Hyun A Gu. Enhanced transdermal deposition and characterization of quercetin-loaded ethosomes. J Chem Eng 2013;3:688-92.

Wang Q, Bao Y, Ahire J, Chao Y. Co-encapsulation of biodegradable nanoparticles with silicon quantum dots and quercetin for monitored delivery. Adv Healthc Mater 2018;3:459-66.

Qi Tan, Weidong Liu, Chenyu Guo, Guangxi Zhai. Preparation and evaluation of quercetin-loaded lecithin-chitosan nanoparticles for topical delivery. Int J Nanomed 2011;6:1621–34.

Soheirn Abd, El Rehamanan, Suhailal, S-Al Jammeel. Quercetin nanoparticles preparation and characterization. Indian J Drug 2014;2:96-103.

Chen Yu G, Chun Fen Y, Qi Lu L. Development of a quercetin-loaded nanostructured lipid carrier formulation for topical delivery. Int J Pharm 2012;2:292-8.

Gulian Quan, In Pan, Zhihua Wang, Qiao Liu Wu. Linghu didan erratum to lactosaminated mesoporous silica nanoparticles for asialoglycoprotein receptor targeted anticancer drug delivery. J Nanobiotechnol 2015;3:83-9.

Avnesh Kumari A, Sudesh Kumar Yadava, Yogesh B, Pakade B, Bikram Singh, Subhash Chandra Yadava. Development of biodegradable nanoparticles for delivery of quercetin. Colloids Surf B Bio Int 2010;80:184–92.

Kumari A, Yadav SK, Pakade YB, Singh B, Yadav SC. Development of biodegradable nanoparticles for delivery of quercetin. Colloids Surf B Biointerfaces 2010;80:184-92.

SB Han, SS Kwon, YM Jeong, ER Yu, SN Park. Physical characterization and in vitro skin permeation of solid lipid nanoparticles for transdermal delivery of quercetin. Int J Cosmetic Sci 2014;36:588-97.

Gurupreet Khandav, DC Bhatt, Deepak Kumar Jindal. Formulation and evaluation of aloplurinol loaded chitosan particles. Int J Appl Pharma 2019;3:49-52.

Ansari KA, Vavia PR, Trotta F, Cavalli R. Cyclodextrin based nanosponges for delivery of resveratrol: in vitro characterization, stability, cytotoxicity, and permeation study. AAPS PharmSciTech 2011;129:279-86.

Sema Saglin, Ugursalgin, Ozgun Vantansever. Synthesis and characterization of beta-cyclodextrin nanosponge and its application for removal of p-nitro phenol from water. Clean Soil Air Water 2015;45:45-56.

Patel J, Trivedi J, Chudhary DS. Microsponges for topical drug delivery. Int J Pharm Res Bio Sci 2014;14:625-38.

Swarupa Arvapally, M Harini, G Harshita. Formulation and in vitro evaluation of glipizide nanosponges. Am J Pharm Tech Res 2017;7:12-32.

Bettini R, Catellani PL, Santi P, Massimo G, Peppas NA, Colombo P. Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate. J Controlled Release 2001;70:383–91.

Cao M, Ren L, Chen G. Formulation optimization and ex vivo and in vivo evaluation of celecoxib microemulsion-based gel for transdermal delivery. AAPS PharmSciTech 2017;18:60–71.

Blanco GarcIa E, Otero Espinar FJ, Blanco M Endez J, Leiro Vidal JM, Luzardo Alvarez A. Development and characterization of anti-inflammatory activity of curcumin-loaded biodegradable microspheres with potential use in intestinal inflammatory disorders. Int J Pharm 2017;12:86-100.

Yinghui Liu, Changshan Sun, Yanru Hao, Gongying Jiang, Li Zheng, Siling Wang. Mechanism of dissolution enhancement and bioavailability of poorly water soluble celecoxib by preparing stable amorphous nanoparticles. J Pharm Pharm Sci 2010;13:589-606.

Geetha Agarwal, Manjil Nagpal, Gurpreet Kaur. Development and comparison of nanosponge and noisome based gel for topical delivery of tazarotene. Pharma Tech 2016;4:213-28.

Jain SK, Chourasia MK, Masuriha R, Soni V, Jain A, Jain NK, et al. Solid lipid nanoparticles bearing flurbiprofen for transdermal delivery. Drug Delivery 2005;12:207–15.

Girish Konadalkar, Asish Dev. Design, development, and evaluation of ion-activated in-situ gel of moxifloxacin hydrochloride. Asian J Pharma Clin Res 2019;3:94-103.

Liu Y, Sun C, Hao Y, Jiang T, Zheng L, Wang S. Mechanism of dissolution enhancement and bioavailability of poorly water-soluble celecoxib by preparing stable amorphous nanoparticles. J Pharm Pharm Sci 2010;13:589–606.

Biswarajan Mohanthy Dipak K, Mujumdar Sagar, MIshra Amulya K Panda. Development and characterization of itracanazole loaded solid lipid nanoparticles. Pharm Dev Tech 2015;20:458-64.

Patil Bhagyashree Subhash, SK Mohite. Formulation design and development of artesunate nanosponges. Eur J Pharma Med Res 2016;3:206-11.

S Jaya, S Divas. Formulation and in vitro evaluation of matrix tablets of metoclopramide hydrochloride. Int J Appl Pharm 2018;11:25-30.

M Tuncay, S Calis, HS Kas M. In vitro and in vivo evaluation of diclofenac sodium loaded albumin microspheres. J Microencapsulation 2000;17:145–55.

Ehab A Found, Alaa Eldeen B Yassin, Hamdan N Alabama. Characterisation of celecoxib loaded solid lipid nanoparticles formulated with tristearin and soft is a 100. Trop J Pharm Res 2015;14:205-10.

Karade P. Formulation, and evaluation of celecoxib gel. J Drug Delivery Ther 2012;2:132-5.

Azadeh Serri, Arash Mahbouli, Afshin Zarghi, Hamid R Moghimi. PAMAM-dendrimer enhanced the antibacterial effect of vancomycin hydrochloride against gram-negative bacteria. J Pharm Pharm Sci 2019;22:10-21.

Abhishek D Dorle, Kumar S Swami, Sujith K Nagare, Supriya R Hyam. Design and evaluation of novel topical gel of tinospora cordifolia as antimicrobial agent Asian J Pharm Clin Res 2015;69:24-34.

Khalid A Anasari, Pradeep R Valli, Franscisco Trota. Roberta cavalla cyclodextrin based nanosponges for delivery of resebertol: in vitro characterization, stability, cytotoxicityand permeation study. AAPS PharmSciTech 2011;12:279-86.

G Jilisha, Vidya Viswanath. Nanosponge loaded hydrogel of cephalexin for topical delivery. Int J Pharm Sci Res 2015;6:27-42.

Lalith Kumar. Novel ethosomal gel of clove oil for treatment of cutaneous candidiasis. J Cosme Dermat 2018;5:21-38.

Koçkaya EA, Selmanoglu G, Kısmet K, Akay MT. Pathological and biochemical effects of therapeutic and supratherapeutic doses of celecoxib in wistar albino male rats. Drug Chem Toxicol 2010;33:410–4.

Auda SH, El-Rasoul SA, Ahmed MM, Osman SK, El-Badry M. In vitro release and in vivo performance of tolmetin from different topical gel formulations. J Pharma Invest 2015;45:311–7.

S Halirfroosh KO. Assessment of celecoxib poly (lactic-glycolic) acid nanoformulation on drug pharmacodynamics and pharmacokinetics in rats. Eur Rev Med Pharmacol Sci 2016;20:4818-29.

L Nikita Sanghavi, SD Bhosale, Yashwant Malode. RP-HPLC method development and validation of quercetin isolated from the plant tridax procumbens. J Sci Innov Res 2014;3:594-7.

Guichen Baohua Hao, Dahong JU. Pharmacokinetic and pharmacodynamic study of triptolide loaded liposome hydrogel patch under micro needles on rats with collagen-induced arthritis. APSB 2015;5:569-76.

Hammam A Mowafy, Fars K Alanazi, Gamal M El Magahraby. Development and validation of an HPLC-UV method for the quantification of carbamazepine in rabbit plasma. Sau Pharm J 2012;3:29-34.

Published

07-09-2019

How to Cite

SUJITHA, Y. S., & MUZIB, Y. I. (2019). FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES. International Journal of Applied Pharmaceutics, 11(5), 156–165. https://doi.org/10.22159/ijap.2019v11i5.32850

Issue

Section

Original Article(s)