Research Journal of Pharmacy and Technology

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Preparation and Evaluation of Eprosartan Mesylate Loaded PLGA Nanostructures


Affiliations
1 Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata,, India
2 Soft Matter and Biophysics Laboratory, Department of Physics, Jadavpur University, Kolkata,, India
     

   Subscribe/Renew Journal


In modern medication, drug-loaded novel polymeric nanoparticles have potential advantages over conventional dosage forms. The present study focused on the formulation development and evaluation of newly introduced angiotensin receptor blocker (ARB) eprosartan mesylate loaded biodegradable acid terminated poly(lactide-co-glycolide) (50:50) nanoparticle using double emulsion solvent evaporation technique. This methodology was found to improve the therapeutic efficacy as Eprosartan Mesylate belongs to BCS class-II and water-insoluble antihypertensive drug with 13% bioavailability. In the earlier stage, screening was performed to find out the suitable combination of excipients (Polyvinyl alcohol, Dichloromethane and Ethanol) to formulate the nanoparticles. In this present study, the physical and chemical properties of polymer and drug were determined before and after the formulation of nanoparticles using experimental techniques, such as Differential Light Scattering (DLS), zeta potential, X-ray Deffractometry (XRD), Fourier-Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Liquid Chromatography-Mass Spectrometry (LC-MS/MS) analysis. The eprosartan mesylate loaded PLGA nanoparticles showed fairly monodispersive, as determined from DLS (average particle diameter 136 nm, Poly Dispesity Index = 0.3). The zeta potential was found to be -10.8mV. This formulation showed a prolonged improved drug release (82.03%) for 360 hours in phosphate buffer (pH7.4) as compared to the conventional marketed dosage form. In-vitro release kinetics data of NPs (R2=0.8979) and diffusion exponent values (n=0.3328) suggested that optimized followed the Korsmeyer-Peppas model with Fickian mechanism.

Keywords

Nanoparticles, Poly Lactic-co-Glycolic Acid (PLGA), Eprosartan Mesylate, Poorly water-soluble drug, Double emulsion-solvent evaporation technique, Controlled release.
Subscription Login to verify subscription
User
Notifications
Font Size


  • R.B. Saudagar, Kanchan T. Mandlik. A Review on Gold Nanoparticles. Asian J. Pharm. Res. 6(1): January -March, (2016); Page 45-48.

  • Catarina Pinto Reis, Ph.D., Ronald J. Neufeld, Ph.D., Antonio J. Ribeiro, Ph.D., Fancisco Veiga, Ph.D., Nanocapsulation I. Method for preparation of drug loaded polymeric nanoparticles (2006), Nanomedicine: Nanotechnology, Biology, and Medicine 2 (2006) 8 – 21.

  • Tzipatly A. Esquivel-Castro, M.C. Ibarra-Alonso, J. Oliva, Antonia Martínez-Luévanos, Porous aerogel and core/shell nanoparticles for controlled drug delivery: A review. Materials Science and Engineering C, (2018).

  • Edyta Swider, Olga Koshkina, Jurjen Tel, Luis J. Cruz, I. Jolanda M. de Vries, Mangala Srinivas, Customizing poly (lactic-co-glycolic acid) particles for biomedical applications, Review article, (2018) Acta Biomaterialia Volume 73, June 2018, Pages 38-51.

  • Sheikh Shafiq, Faiyaz Shakeel, Sushma Talegaonkar, Farhan J. Ahmad, Roop K. Khar, Mushir Ali, Development and bioavailability assessment of ramipril nanoemulsion formulation, (2006), European Journal of Pharmaceutics and Biopharmaceutics 66 (2007) 227–243.

  • Murugesan Sathiya Deepikaa, Ramar Thangamb, Thankaraj Salammal Sheenac, R.T.V. Vimalad, Srinivasan Sivasubramanianb, Kulandaivel Jeganathanc, Ramasamy Thirumurugana, Dual drug loaded PLGA nanospheres for synergistic efficacy in breast cancer therapy, (2019), Materials Science and Engineering. C, Materials for Biological Applications [02 May 2019, 103:109716], Type: Journal Article.

  • Shekhawat Prachia, Bagul Milindb, Edwankar Dipteeb, Pokharkar Varshaa, Enhanced dissolution/caco-2 permeability, pharmacokinetic and pharmacodynamic performance of re-dispersible eprosartan mesylate nano powder, European Journal of Pharmaceutical Sciences 132 (2019) 72–85.

  • Pandya Dimple Bhupendra, Shinkar Dattatraya Manohar, Saudagar Ravindra Bhanudas, Bacchav Jyoti Kailas, UV Spectrophotometric Method for Estimation of Eprosartan Mesylate in Bulk and in Pharmaceutical Formulation, Asian J. Pharm. Ana. (2016); 6(2): 119-121.

  • Mohammed M. Abdol Quader, Mohamed A. Osman, Gamal M. El Maghraby, Intestinal Absorption Of Eprosartan Mesylate From Self Emulsifying System And Cyclodextrin Complex, (2017) International Journal of Pharmacy and Pharmaceutical Sciences, ISSN- 0975-1491 Vol 9, Issue 2, 2017.

  • P. J. Blankestijn and H. Rupp, Clinical Profile of Eprosartan: A Different Angiotensin II Receptor Blocker, Cardiovascular and Hematological Agents in Medicinal Chemistry, (2008), 6, 253-257.

  • Xue-Ning Li, Hong-Rong Xu, Wei-Li Chen, Gang-Yi Liu, Nan-Nan Chu, Chen Yu, Determination of eprosartan in human plasma and urine by LC/MS/MS, Journal of Chromatography B, 853 (2007) 47–53.

  • Ravi Kumar Trivedi, Raja Reddy Kallem, Ramesh Mullangi, Nuggehally R. Srinivas, Simultaneous determination of rosuvastatin and fenofibric acid in human plasma by LC–MS/MS with electrospray ionization, Assay development, validation and application to a clinical study, J Pharm Biomed Anal. (2005) Sep 15;39(3-4):661-9.

  • Fabienne Danhier, Eduardo Ansorena, Joana M. Silva, Régis Coco, Aude Le Breton, Véronique Préat, PLGA-based nanoparticles: An overview of biomedical applications, Journal of Controlled Release 161 (2012) 505–522.

  • S. Sathish Kumar, G. Melchias, P. Ravikumar, R. Chandrasekar and P. Kumaravel, Bioinspired synthesis of silver nanoparticles using Euphorbia hirta leaf extracts and their antibacterial activity, Asian J. Pharm. Res. 4(1): Jan.-Mar. (2014); Page 39-43.

  • Anilkumar J Shinde, Harinath N More. Nanoparticles: As Carriers for Drug Delivery System . Research J. Pharma. Dosage Forms and Tech. (2009); 1(2): 80-86 . 16. Sonali P. Mahaparale, Reshma S. Kore. Silver Nanoparticles: Synthesis, Characterization, Application, Future Outlook. Asian J. Pharm. Res. (2019); 9(3):181-189.

  • M. Najlah, Z. Ahmed, M. Iqbal, Z. Wang, P. Tawari, W. Wang, C. McConville, Development and Characterisation of Disulfiram-loaded PLGA Nanoparticles for the Treatment of Non-Small Cell Lung Cancer, European Journal of Pharmaceutics and Biopharmaceutics (2016), vol. 112, EJPB 12367, pp. 224-233.

  • Luo, Y., Teng, Z., Li, Y., and Wang, Q., Solid lipid nanoparticles for oral drug delivery: chitosan coating improves stability, controlled delivery, mucoadhesion and cellular uptake, Carbohydrate Polymers (2015).

  • Prashant S. Wake, Dr. M. D. Kshirsagar, Compatibility study In-vitro drug release Study of Solid Lipid Nanoparticle Based Transdermal Drug Delivery System for Rasagiline Mesylate. Asian J. Res. Pharm. Sci. (2017); 7(2): 92-96.

  • Dipika Mandal, Tapan Kumar Shaw, Goutam Dey, Murari Mohan Pal, Biswajit Mukherjee, Amal Kumar Bandyopadhyay, Mahitosh Mandal, Preferential hepatic uptake of paclitaxel-loaded poly-(d-l-lactide-co-glycolide) nanoparticles — A possibility for hepatic drug targeting: Pharmacokinetics and biodistribution. Biomac (2017).

  • Subir Kumar Patla, Ruma Ray, K. Asokan, and Sanat Karmakar, Investigation of ionic conduction in PEO–PVDF based blend polymer electrolytes, Journal of Applied Physics (2018).

  • Pradipta Sarkar, Saswati Bhattacharya and Tapan Kumar Pal, Application of statistical design to evaluate critical process parameters and optimize formulation technique of polymeric nanoparticles, (2019) R. Soc. open sci. 6: 190896.

  • Saswati Bhattacharya, Jasmina Khanam, Pradipta Sarkar, and Tapan Kumar Pal, A chemotherapeutic approach targeting the acidic tumor microenvironment: combination of a proton pumps inhibitor and paclitaxel for statistically optimized nanotherapeutics, RSC Advances (2018).

  • Ashok. P, Meyyanathan. S. N, R. Vadivelan, Jawahar. N. Nanosuspensions by Solid Lipid Nanoparticles method for the Formulation and in vitro/in vivo characterization of Nifedipine. Asian J. Res. Pharm. Sci. (2021); 11(1):1-6.

  • Ashok P., Meyyanathan S. N., Jawahar N., R. Vadivelan. Irbesartan Formulation and Evaluation of Loaded Solid Lipid Nanoparticles by Microemulsion Techinque. Asian J. Pharm. Tech. 2020; 10(4):228-230.

  • Ismaiel A Tekko, Ola M Ali, Taher Hatahet and Mustafa F Chehna, Polyethylene Glycol-Based Solid Dispersions to Enhance Eprosartan Mesylate Dissolution and Bioavailability, Archives of Pharmacy and Pharmacology Research, Published date: November 07, (2019).

  • Rohan R. Vakhariya, Swati S. Talokar, V. R. Salunkhe, C. S. Magdum. Formulation Development and Optimization of Simvastatin Loaded Solid Lipid Nanoparticles. Asian J. Res. Pharm. Sci. (2017); 7(1): 49-52.

  • Pankaj Vijay Dangre, Mangesh Dinanath Godbole, Priyanka Vijay Ingale, Debarshi Kar Mahapatra, Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods, Indian Journal of Pharmaceutical Education and Research, Vol 50, Issue 3, Jul-Sep (Suppl.), (2016).

  • Muddana E.B. Rao, Suryakanta Swain, Chinam N. Patra and Shakti P. Mund, Formulation Design, Optimization and Characterization of Eprosartan Mesylate Nanoparticles, Nanoscience and Nanotechnology-Asia, (2018), 8, 130-143.

  • Kandasamy Saravanakumara, Xiaowen Hua, Sabarathinam Shanmugamb, Ramachandran Chelliahc, Ponarulselvam Sekarb, Deog-Hwan Ohc, Sekar Vijayakumara, Kandasamy Kathiresand, Myeong-Hyeon Wanga, Enhanced cancer therapy with pH-dependent and aptamer functionalized doxorubicin loaded polymeric (poly D, L-lactic-co-glycolic acid) nanoparticles, Archives of Biochemistry and Biophysics 671 (2019) 143–151.

  • M. Iqbal et al. Double emulsion solvent evaporation techniques used for drug encapsulation International Journal of Pharmaceutics 496 (2015) 173–190

  • C.I.C. Crucho, M.T. Barros, Polymeric nanoparticles: A study on the preparation variables and characterization methods, Materials Science and Engineering C 80 (2017),773, 771–784.

  • C.X. Song, V. Labhasetwar, H. Murphy, X. Qu, W.R. Humphrey, R.J. Shebuski, R.J. Levya, Formulation and characterization of biodegradable nanoparticles for intravascular local drug delivery, Journal of Controlled Release 43 (1997) 197–212.

  • Pranab Jyoti Das, Paramita Paul, Biswajit Mukherjee, Bhaskar Mazumder, Laboni Mondal, Rinku Baishya, Mita Chatterjee Debnath, and Kumar Saurav Dey, Pulmonary Delivery of Voriconazole Loaded Nanoparticles Providing A Prolonged Drug Level in Lungs- A Promise for Treating Fungal Infection, Mol. Pharmaceutics, (2015).

  • J. Prasad Raoa, Kurt E. Geckeler, Polymer nanoparticles: Preparation techniques

  • and size-control parameters, Progress in Polymer Science 36 (2011) 887–913. 36. Yu Zhang and Mo Yang and Nathaniel G. Portney and Daxiang Cui and Gurer Budak and Ekmel Ozbay and Mihrimah Ozkan and Cengiz S. Ozkan, Zeta potential: a surface electrical characteristic to probe the interaction of nanoparticles with normal and cancer human breast epithelial cells, Biomed Microdevices (2008) 10:321–328.

  • Namdev L. Dhas, Pradum P. Ige Ritu R. Kudarha, Design, Optimization and in-vitro study of Folic acid Conjugated-Chitosan Functionalized PLGA Nanoparticle for Delivery of Bicalutamide in Prostate Cancer, Powder Technology (2015).

  • Avinash B Darekar, Sonali N Jadhav, Ravindra B Saudagar, Design Development and Evaluation of Bilayer Tablet Using Eprosartan Mesylate for the Treatment of Hypertension, International Journal of Current Pharmaceutical Review and Research; 8(4); 328-337, IJCPR, Volume 8, Issue 4, July - August (2017)

  • T. Musumeci, C.A. Ventura, I. Giannone a, B. Ruozi, L. Montenegro, R. Pignatello, G. Puglisi, PLA/PLGA nanoparticles for sustained release of docetaxel, International Journal of Pharmaceutics 325 (2006) 172–179

  • Ravi Sharma, D.P. Bisen, Usha Shukla and B.G. Sharma, X-ray diffraction: a powerful method of characterizing nanomaterials, Recent Research in Science and Technology (2012), 4(8): 77-79

  • Jae Soon Ahn, Kang Min Kim, Chan Young Ko and Jae Seon Kang, Absorption Enhancer and Polymer (Vitamin E TPGS and PVP K29) by Solid Dispersion Improve Dissolution and Bioavailability of Eprosartan Mesylate, Bull. Korean Chem. Soc. (2011), Vol.32, No.5 1587.

  • Avinash Budhian, Steven J. Siegel, Karen I. Winey, Controlling the in vitro release profiles for a system of haloperidol-loaded PLGA nanoparticles, International Journal of Pharmaceutics 346 (2008) 151–159.

  • Superb K. Misra, Agnieszka Dybowska, Deborah Berhanu, Samuel N. Luoma c, Eugenia Valsami-Jones, The complexity of nanoparticle dissolution and its importance in nanotoxicological studies, Science of the Total Environment 438 (2012) 225–232.

  • G. Mittal, D.K. Sahana, V. Bhardwaj, M.N.V. Ravi Kumar, Estradiol loaded PLGA nanoparticles for oral administration: Effect of polymer molecular weight and copolymer composition on release behavior in vitro and in vivo, Journal of Controlled Release 119 (2007) 77–85.

  • Ahmed S. Hussein, Norhafizah Abdullah, Fakhru’l-Razi Ahmadun, In vitro degradation of poly (D, L lactide-co-glycolide) nanoparticles loaded with linamarin, IET Nanobiotechnol., (2013), Vol. 7, Iss. 2, pp. 33–41 33.

  • Choudhury A, Dash SK , Roy A, Bahadur S, Saha S, Das S. Design and Evaluation of Ranitidine Hydrochloride Floating Tablets for oral controlled release. Research J. Pharma. Dosage Forms and Tech. (2009); 1(2): 167-170.


Abstract Views: 144

PDF Views: 0




  • Preparation and Evaluation of Eprosartan Mesylate Loaded PLGA Nanostructures

Abstract Views: 144  |  PDF Views: 0

Authors

Easha Biswas
Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata,, India
Sanmoy Karmakar
Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata,, India
Tapan Kumar Pal
Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata,, India
Kalyan Kumar Banerjee
Soft Matter and Biophysics Laboratory, Department of Physics, Jadavpur University, Kolkata,, India
Sanat Karmakar
Soft Matter and Biophysics Laboratory, Department of Physics, Jadavpur University, Kolkata,, India

Abstract


In modern medication, drug-loaded novel polymeric nanoparticles have potential advantages over conventional dosage forms. The present study focused on the formulation development and evaluation of newly introduced angiotensin receptor blocker (ARB) eprosartan mesylate loaded biodegradable acid terminated poly(lactide-co-glycolide) (50:50) nanoparticle using double emulsion solvent evaporation technique. This methodology was found to improve the therapeutic efficacy as Eprosartan Mesylate belongs to BCS class-II and water-insoluble antihypertensive drug with 13% bioavailability. In the earlier stage, screening was performed to find out the suitable combination of excipients (Polyvinyl alcohol, Dichloromethane and Ethanol) to formulate the nanoparticles. In this present study, the physical and chemical properties of polymer and drug were determined before and after the formulation of nanoparticles using experimental techniques, such as Differential Light Scattering (DLS), zeta potential, X-ray Deffractometry (XRD), Fourier-Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Liquid Chromatography-Mass Spectrometry (LC-MS/MS) analysis. The eprosartan mesylate loaded PLGA nanoparticles showed fairly monodispersive, as determined from DLS (average particle diameter 136 nm, Poly Dispesity Index = 0.3). The zeta potential was found to be -10.8mV. This formulation showed a prolonged improved drug release (82.03%) for 360 hours in phosphate buffer (pH7.4) as compared to the conventional marketed dosage form. In-vitro release kinetics data of NPs (R2=0.8979) and diffusion exponent values (n=0.3328) suggested that optimized followed the Korsmeyer-Peppas model with Fickian mechanism.

Keywords


Nanoparticles, Poly Lactic-co-Glycolic Acid (PLGA), Eprosartan Mesylate, Poorly water-soluble drug, Double emulsion-solvent evaporation technique, Controlled release.

References