Login Register Cart 0
Generic placeholder image

Current Applied Materials

Editor-in-Chief

ISSN (Print): 2666-7312
ISSN (Online): 2666-7339

Back
Journal Home About Journal Editorial Board Current Issue Volumes/Issues
Subscribe
Research Article

Development and Optimization of Polymeric Nanoparticles and their In vitro Deposition Studies Using Modified TSI

Author(s): Bhushan R. Rane, Pranit S. Waghchaure, Akash J. Amkar* and Ashish R. Jain

Volume 3, 2024

Published on: 04 April, 2024

Article ID: e040424228641 Pages: 12

DOI: 10.2174/0126667312289623240327073342

Price: $65

Abstract

Background: To deliver the drug through the pulmonary route, polymers like oleoylcarboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methylcellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have the potential for a therapeutic response for the targeted site is a beneficial approach.

Objective: The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to develop the PNPs for pulmonary delivery.

Methods: Polymeric nanoparticles are developed by homogenization and solvent evaporation methods and characterized by modified twin-stage impinger to study in vitro deposition.

Results: The characterization of pirfenidone-loaded polymeric nanoparticles (PFD-PNPs) reveals that the mean particle size of O-CMC-PNPs is 140.8 nm ± 20, found to be less than CS-PNPs and HPMC-PNPs. The polydispersibility index reveals that the particles of all prepared formulations are homogenous. At the same time, the zeta potential of O-CMC-PNPs is 40.8 mV ± 5.64, and the entrapment efficiency is 91% ± 1.2, which is better as compared to Chitosan and HPMC K4M PNPs and makes them efficient for pulmonary delivery. Findings from the in vitro deposition study using modified TSI show that 88.5% of the drug delivered through nebulization from both the stage of right and left sides of the TSI suggests effective deposition in the lungs of O-CMC PNPs, and it may move to the deeper regions because of the lowest diameter of the particles. Sustaining release of the drug was found in the O-CMC PNPs for 8 hours, compared with 5 and 7 hours for HPMC PNPs and Chitosan PNPs, respectively.

Conclusions: Overall, the results of the O-CMC-PNPs highlight that the prepared nanoparticles with O-CMC would be effective for pulmonary delivery instead of chitosan and HPMC K4M.

[1]
Su S. M Kang P, Recent Advances P. Recent advances in nanocarrier-assisted therapeutics delivery systems. Pharmaceutics 2020; 12(9): 837.
[http://dx.doi.org/10.3390/pharmaceutics12090837] [PMID: 32882875]
[2]
Li F, Qin Y, Lee J, et al. Stimuli-responsive nano-assemblies for remotely controlled drug delivery. J Control Release 2020; 322: 566-92.
[http://dx.doi.org/10.1016/j.jconrel.2020.03.051] [PMID: 32276006]
[3]
Banik BL, Fattahi P, Brown JL. Polymeric nanoparticles: The future of nanomedicine. Wiley Interdiscip Rev Nanomed Nanobiotechnol 2016; 8(2): 271-99.
[http://dx.doi.org/10.1002/wnan.1364] [PMID: 26314803]
[4]
Wilczewska AZ, Niemirowicz K, Markiewicz KH, Car H. Nanoparticles as drug delivery systems. Pharmacol Rep 2012; 64(5): 1020-37.
[http://dx.doi.org/10.1016/S1734-1140(12)70901-5] [PMID: 23238461]
[5]
Bakshi PS, Selvakumar D, Kadirvelu K, Kumar NS. Chitosan as an environment friendly biomaterial – a review on recent modifications and applications. Int J Biol Macromol 2019; 150: 1072.
[http://dx.doi.org/10.1016/j.ijbiomac.2019.10.113] [PMID: 31739057]
[6]
Mikušová V, Mikuš P. Advances in chitosan-based nanoparticles for drug delivery. Int J Mol Sci 2021; 22(17): 9652.
[http://dx.doi.org/10.3390/ijms22179652] [PMID: 34502560]
[7]
Mašková E, Kubová K, Raimi-Abraham BT, et al. Hypromellose – A traditional pharmaceutical excipient with modern applications in oral and oromucosal drug delivery. J Control Release 2020; 324: 695-727.
[http://dx.doi.org/10.1016/j.jconrel.2020.05.045] [PMID: 32479845]
[8]
Lim C, Hwang DS, Lee DW. Intermolecular interactions of chitosan: Degree of acetylation and molecular weight. Carbohydr Polym 2021; 259: 117782.
[http://dx.doi.org/10.1016/j.carbpol.2021.117782] [PMID: 33674019]
[9]
Lim C, Lee DW, Israelachvili JN, Jho Y, Hwang DS. Contact time- and pH-dependent adhesion and cohesion of low molecular weight chitosan coated surfaces. Carbohydr Polym 2015; 117: 887-94.
[http://dx.doi.org/10.1016/j.carbpol.2014.10.033] [PMID: 25498713]
[10]
Tian Y, Sun Y, Wang X. Chitosan and its derivatives-based nanoformulations in drug delivery. Nanobiomaterials in Drug Delivery Applications of Nanobiomaterials. Amsterdam: Elsevier 2016; 9: pp. 515-72.
[http://dx.doi.org/10.1016/B978-0-323-42866-8.00015-0]
[11]
Biswas S, Ahmed T. Biomedical applications carboxymethyl chitosans. Handbook of Chitin and Chitosan. Amsterdam: Elsevier 2020; 3: pp. 433-70.
[http://dx.doi.org/10.1016/B978-0-12-817966-6.00014-5]
[12]
Na HN, Park SH, Kim K-I, Kim MK, Son T-I. Photocurable O-carboxymethyl chitosan derivatives for biomedical applications: Synthesis, in vitro biocompatibility, and their wound healing effects. Macromol Res 2012; 20(11): 1144-9.
[http://dx.doi.org/10.1007/s13233-012-0167-2]
[13]
Ameeduzzafar Ali J, Bhatnagar A, Kumar N, Ali A. Chitosan nanoparticles amplify the ocular hypotensive effect of cateolol in rabbits. Int J Biol Macromol 2014; 65: 479-91.
[http://dx.doi.org/10.1016/j.ijbiomac.2014.02.002] [PMID: 24530326]
[14]
Attri K, Singh M, Sharma K, Srivastav S, Sharma L, Bhalla V. A review on recent trends in nasal drug delivery system. Ann Rom Soc Cell Biol 2022; 26(1): 1038-56.
[15]
Labiris NR, Dolovich MB. Pulmonary drug delivery. Part I: Physiological factors affecting therapeutic effectiveness of aerosolized medications. Br J Clin Pharmacol 2003; 56(6): 588-99.
[http://dx.doi.org/10.1046/j.1365-2125.2003.01892.x] [PMID: 14616418]
[16]
Hussain M, Madl P, Khan A. Lung deposition predictions of airborne particles and the emergence of contemporary diseases, Part-I. Health 2011; 2(2): 51-9.
[17]
Longest W, Spence B, Hindle M. Devices for improved delivery of nebulized pharmaceutical aerosols to the lungs. J Aerosol Med Pulm Drug Deliv 2019; 32(5): 317-39.
[http://dx.doi.org/10.1089/jamp.2018.1508] [PMID: 31287369]
[18]
EMA. Access to documents. 2022. Available From: https://www.ema.europa.eu/en/about-us/how-we-work/access-documents
[19]
Lyseng-Williamson KA. Pirfenidone tablets in idiopathic pulmonary fibrosis: A profile of their use. Drugs Ther Perspect 2018; 34(1): 8-15.
[http://dx.doi.org/10.1007/s40267-017-0459-x] [PMID: 30008572]
[20]
Taniguchi H, Ebina M, Kondoh Y, et al. Pirfenidone in idiopathic pulmonary fibrosis. Eur Respir J 2010; 35(4): 821-9.
[http://dx.doi.org/10.1183/09031936.00005209] [PMID: 19996196]
[21]
Kim ES, Keating GM. Pirfenidone: A review of its use in idiopathic pulmonary fibrosis. Drugs 2015; 75(2): 219-30.
[http://dx.doi.org/10.1007/s40265-015-0350-9] [PMID: 25604027]
[22]
Fujiwara A, Funaki S, Fukui E, et al. Effects of pirfenidone targeting the tumor microenvironment and tumor-stroma interaction as a novel treatment for non-small cell lung cancer. Sci Rep 2020; 10(1): 10900.
[http://dx.doi.org/10.1038/s41598-020-67904-8] [PMID: 32616870]
[23]
Parmar VK, Desai SB, Vaja T. RP-HPLC and UV spectrophotometric methods for estimation of pirfenidone in pharmaceutical formulations. Indian J Pharm Sci 2014; 76(3): 225-9.
[PMID: 25035534]
[24]
Chen X, Wang T. Preparation and characterization of atrazine-loaded biodegradable PLGA nanospheres. J Integr Agric 2019; 18(5): 1035-41.
[http://dx.doi.org/10.1016/S2095-3119(19)62613-4]
[25]
Kakad SP, Gangurde TD, Kshirsagar SJ, Mundhe VG. Nose to brain delivery of nanosuspensions with first line antiviral agents is alternative treatment option to Neuro-AIDS treatment. Heliyon 2022; 8(7): e09925.
[http://dx.doi.org/10.1016/j.heliyon.2022.e09925] [PMID: 35879999]
[26]
Mulia K, Safiera A, Pane IF, Krisanti EA. Effect of high speed homogenizer speed on particle size of polylactic acid. J Phys Conf Ser 2019; 1198(6): 062006.
[http://dx.doi.org/10.1088/1742-6596/1198/6/062006]
[27]
Md S, Kuldeep Singh JKAP, Waqas M, et al. Nanoencapsulation of betamethasone valerate using high pressure homogenization–solvent evaporation technique: Optimization of formulation and process parameters for efficient dermal targeting. Drug Dev Ind Pharm 2019; 45(2): 323-32.
[http://dx.doi.org/10.1080/03639045.2018.1542704] [PMID: 30404554]
[28]
Pandit J, Sultana Y, Aqil M. Chitosan-coated PLGA nanoparticles of bevacizumab as novel drug delivery to target retina: Optimization, characterization, and in vitro toxicity evaluation. Artif Cells Nanomed Biotechnol 2017; 45(7): 1397-407.
[http://dx.doi.org/10.1080/21691401.2016.1243545] [PMID: 27855494]
[29]
Omar Zaki SS, Ibrahim MN, Katas H. Particle size affects concentration-dependent cytotoxicity of chitosan nanoparticles towards mouse hematopoietic stem cells. J Nanotechnol 2015; 2015: 1-5.
[http://dx.doi.org/10.1155/2015/919658]
[30]
Korbag I, Mohamed Saleh S. Studies on the formation of intermolecular interactions and structural characterization of polyvinyl alcohol/lignin film. Int J Environ Stud 2016; 73(2): 226-35.
[http://dx.doi.org/10.1080/00207233.2016.1143700]
[31]
Alsaidan OA, Pattanayak P, Awasthi A, et al. Quality by design-based optimization of formulation parameters to develop quercetin nanosuspension for improving its biopharmaceutical properties. S Afr J Bot 2022; 149: 798-806.
[http://dx.doi.org/10.1016/j.sajb.2022.04.030]
[32]
Jarrar QB, Hakim MN, Cheema MS, Zakaria ZA. In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes. Braz J Pharm Sci 2019; 55(12): 18.
[33]
Zafar A, Alruwaili NK, Imam SS, et al. Development and optimization of hybrid polymeric nanoparticles of apigenin: Physicochemical characterization, antioxidant activity and cytotoxicity evaluation. Sensors (Basel) 2022; 22(4): 1364.
[http://dx.doi.org/10.3390/s22041364] [PMID: 35214260]
[34]
Owodeha-Ashaka K, Ilomuanya MO, Iyire A. Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery. Prog Biomater 2021; 10(3): 207-20.
[http://dx.doi.org/10.1007/s40204-021-00164-5] [PMID: 34549376]
[35]
Michailidou G, Ainali NM, Xanthopoulou E, et al. Effect of poly(vinyl alcohol) on nanoencapsulation of budesonide in chitosan nanoparticles via ionic gelation and its improved bioavailability. Polymers (Basel) 2020; 12(5): 1101.
[http://dx.doi.org/10.3390/polym12051101] [PMID: 32408557]
[36]
Bhattacharjee S. DLS and zeta potential – What they are and what they are not? J Control Release 2016; 235: 337-51.
[http://dx.doi.org/10.1016/j.jconrel.2016.06.017] [PMID: 27297779]
[37]
Ali NA, Kishta MS, Fekry M, Mohamed SH. The targeted delivery of chitosan nanoparticles to treat indoxacarb: Induced lung fibrosis in rats. Bull Natl Res Cent 2022; 46(1): 274.
[http://dx.doi.org/10.1186/s42269-022-00963-1]
[38]
Rane BR, Gujarathi NA, Patel JK. Biodegradable anionic acrylic resin based hollow microspheres of moderately water soluble drug Rosiglitazone Maleate: Preparation and in vitro characterization. Drug Dev Ind Pharm 2012; 38(12): 1460-9.
[http://dx.doi.org/10.3109/03639045.2011.653811] [PMID: 22356275]
[39]
Gujarathi NA, Rane BR, Patel JK. pH sensitive polyelectrolyte complex of O-carboxymethyl chitosan and poly (acrylic acid) cross-linked with calcium for sustained delivery of acid susceptible drugs. Int J Pharm 2012; 436(1-2): 418-25.
[http://dx.doi.org/10.1016/j.ijpharm.2012.07.016] [PMID: 22814224]
[40]
Sohail A, Khan RU, Khan M, et al. Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica. Bull Natl Res Cent 2021; 45(1): 187.
[http://dx.doi.org/10.1186/s42269-021-00644-5]
[41]
Debnath SK, Saisivam S, Debanth M, Omri A. Development and evaluation of Chitosan nanoparticles based dry powder inhalation formulations of Prothionamide. PLoS One 2018; 13(1): e0190976.
[http://dx.doi.org/10.1371/journal.pone.0190976] [PMID: 29370192]
[42]
Pourshahab PS, Gilani K, Moazeni E, Eslahi H, Fazeli MR, Jamalifar H. Preparation and characterization of spray dried inhalable powders containing chitosan nanoparticles for pulmonary delivery of isoniazid. J Microencapsul 2011; 28(7): 605-13.
[http://dx.doi.org/10.3109/02652048.2011.599437] [PMID: 21793647]
[43]
Nasibi S. Nargesi khoramabadi H, Arefian M, et al. A review of Polyvinyl alcohol/Carboxiy methyl cellulose (PVA/CMC) composites for various applications. Journal of Composites and Compounds 2020; 2(3): 68-75.
[http://dx.doi.org/10.29252/jcc.2.2.2]
[44]
Gilani K, Moazeni E, Ramezanli T, Amini M, Fazeli MR, Jamalifar H. Development of respirable nanomicelle carriers for delivery of amphotericin B by jet nebulization. J Pharm Sci 2011; 100(1): 252-9.
[http://dx.doi.org/10.1002/jps.22274] [PMID: 20602350]
[45]
Sharma M, Sharma R, Jain DK, Saraf A. Enhancement of oral bioavailability of poorly water soluble carvedilol by chitosan nanoparticles: Optimization and pharmacokinetic study. Int J Biol Macromol 2019; 135: 246-60.
[http://dx.doi.org/10.1016/j.ijbiomac.2019.05.162] [PMID: 31128197]

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy