Abstract
The goal of the current investigation was to prepare PEGylated Lipova E120 liposomes loaded with celecoxib for the effective treatment of rheumatoid arthritis (RA). PEGylated liposomes were prepared and were characterized using techniques such as particle size distribution, polydispersity index (PDI), zeta potential, encapsulation efficiency and in-vitro release, in-vivo and stability studies. The morphological study was characterized by scanning electron microscopy and transmission electron microscopy. To determine the interaction between drug and polymer Fourier transform infrared, Raman, thermogravimetric analysis and differential scanning calorimetry studies were performed. Results show that formulation F6 was optimized with a particle size of 92.12 ± 1.7 nm, a PDI of 0.278 ± 0.22, a zeta potential of − 40.8 ± 1.7 mV with a maximum encapsulation of 96.6 ± 0.05% of drug in the PEGylated liposomes. The optimized formulation shows a maximum release of drug i.e. 94.45 ± 1.13% in 72 h. Tail immersion assay shows that the optimized formulation F6 significantly increases the reaction time and carrageenan-induced assay shows that the optimized formulation inhibits the increase in paw edema thus providing a pain relief treatment in RA. These results suggest that the PEGylated liposomes provide a sustained release of celecoxib and helps in effective treatment of RA.
Similar content being viewed by others
References
Ahlmen M, Svensson B, Albertsson K, Forslind K and Hafstrom I 2010 Influence of gender on assessments of disease activity and function in early rheumatoid arthritis in relation to radiographic joint damage. Ann. Rheum. Dis. 69 230–233
Alavi SE, Esfahani MKM, Ghassemi S, Akbarzadeh A and Hassanshahi G 2014 In vitro evaluation of the efficacy of liposomal and Pegylated liposomal hydroxyurea. Indian J. Clin. Biochem. 29 84–88
Atyabi F, Farkhondehfai A, Esmaeil F and Dinarvand R 2009 Preparation of PEGylated nano-liposomal formulation containing SN-38: In vitro characterization and in vivo biodistribution in mice. Acta Pharm. 59 133–144
Begum YM, Abbulu K and Sudhakar M 2012 Celecoxib loaded liposome: Development, characterization and in vitro evaluation. Int. J. Pharm. Sci. Res. 3 154–161
Betageri GV and Parsons DL 1992 Drug encapsulation and release from multilamellar and unilamellar liposomes. Int. J. Pharm. 81 235–241
Bhalerao SS and Harshal AR 2003 Preparation, optimization, characterization and stability studies of salicyclic acid liposomes. Drug Dev. Ind. Pharm. 29 457–467
Cheow WS, Chang MW and Hadinoto K 2011 The roles of lipid in anti-biofilm efficacy of lipid–polymer hybrid nanoparticles encapsulating antibiotics. Colloids Surf., A 389 158–165
Dave V, Sharma S, Yadav RB and Agarwal U 2017a Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis. Appl. Nanosci. 7 973–987
Dave V, Yadav RB, Kushwaha K, Yadav S, Sharma S and Agrawal U 2017b Lipid-polymer hybrid nanoparticles: Development & statistical optimization of norfloxacin for topical drug delivery system. Bioact. Mater. 2 269–280
Er Y, Barnes TJ, Fornasiero D and Fornasiero CA 2009 The encapsulation and release of guanosine from PEGylated liposomes. J. Liposome Res. 19 29–36
Gibofsky A 2012 Overview of epidemiology, pathophysiology and diagnosis of rheumatoid arthritis. Am. J. Manag. Care 18 295–302
Goldenberg MM 1999 Celecoxib, a selective cyclooxygenase-2 inhibitor for the treatment of rheumatoid arthritis and osteoarthritis. Clin. Ther. 21 1497–1513
Jain NK and Kulkarni SK 1999 Antinociceptive and anti-inflammatory effects of Tanacetum parthenium L. extract in mice and rats. J. Ethnopharmacol. 68 251–259
Kahlenberg JM and Fox DA 2011 Advances in the medical treatment of rheumatoid arthritis. Hand Clin. 27 11–20
Kaiser N, Kimpfler A, Massing U, Burger AM, Fiebig HH, Brandl M and Schubert R 2003 5-Fluorouracil in vesicular phospholipid gels for anticancer treatment: Entrapment and release properties. Int. J. Pharm. 256 123–131
Li J, Wang X, Zhang T, Wang C, Huang Z, Luo X and Deng Y 2015 A review on phospholipids and their main applications in drug delivery systems. Asian J. Pharm. Sci. 10 81–98
McCormack PL 2011 Celecoxib: A review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and anklosing spondylitis. Drugs 71 2457–2489
Naveed S, Sultana N and Arayne MS 2014 In vivo interaction studies of lisinopril with flurbiprofen and ibuprofen on carrageenan induced inflammation. J. Bioanal. Biomed. 6 1–4
Panwar P, Pandey B, Lakhera PC and Singh KP 2010 Preparation, characterization, and in vitro release study of albendazole-encapsulated nanosize liposomes. Int. J. Nanomed. 5 101–108
Rathode S and Deshpande SG 2010 Design and evaluation of liposomal formulation of Pilocarpine nitrate. Indian J. Pharm. Sci. 72 155–160
Re F, Cambianica I, Zona C, Sesana S, Gregori M, Rigolio R, La Ferla B, Nicotra F, Forloni G, Cagnotto A, Salmona M, Masserini M and Sancini G 2011 Functionalization of liposomes with ApoE-derived peptides at different density affects cellular uptake and drug transport across a blood-brain barrier model. Nanomed. Nanotechnol. Biol. Med. 7 551–559
Rengel RG, Barišić K, Pavelić Ž, Grubisic TZ, Cepelak I and Filipovic-Grcic J 2002 High efficiency entrapment of superoxide dismutase into mucoadhesive chitosan-coated liposomes. Eur. J. Pharm. Sci. 5 441–448
Sant VP and Nagarsenker MS 2011 Synthesis of monomethoxy polyethylene glycol-cholesteryl ester and effect of its incorporation in liposomes. AAPS PharmSciTech 12 1056–1063
Sercombe L, Veerati T, Moheimani F, Wu SY, Sood AK and Hua S 2015 Advances and challenges of liposome assisted drug delivery. Front. Pharmacol. 6 286
Sharma P, Pant S, Rai S, Yadav RB and Dave V 2017 Green synthesis and characterization of silver nanoparticles by Allium cepa L. to produce silver nano‐coated fabric and their antimicrobial evaluation. Appl. Orgnomet. Chem. 32 1–13
Shavi GV, Reddy MS, Raghavendra R, Nayak UY, Kumar AR, Deshpande PB, Udupa N, Behl G, Dave V and Kushwaha K 2016 PEGylated liposomes of anastrozole for long-term treatment of breast cancer: in vitro and in vivo evaluation. J. Liposome Res. 26 28–46
Siebert S, Lyall DM, Mackay DF, Porter D, McInnes IB, Sattar N and Pell JP 2016 Characteristics of rheumatoid arthritis and its association with major comorbid conditions: cross-sectional study of 502 649 UK Biobank participants. RMD Open 2 1–10
Sofidiyaa MO, Imeha E, Ezeania C, Aigbeb FR and Akindele AJ 2014 Antinociceptive and anti-inflammatory activities of ethanolic extract of Alafia barteri. Rev. Bras. Farmacogn. 24 348–354
Wang X, Song Y, Su Y, Tian Q, Li B, Quan J and Deng Y 2016 Are PEGylated liposomes better than conventional liposomes? A special case for vincristine. Drug Delivery 23 1092–1100
Yalcin TE, Ilbasmis-Tamer S, Ibisoglu B, Özdemir A, Ark M and Takka S 2017 Gemcitabine hydrochloride-loaded liposomes and nanoparticles: Comparison of encapsulation efficiency, drug release, particle size, and cytotoxicity. Pharm. Dev. Technol. 23 76–86
Acknowledgements
The authors acknowledge VAV Life Sciences Pvt Ltd, Mumbai, Maharashtra for providing a gift sample of polymer and their generous support throughout the research work.
Author information
Authors and Affiliations
Corresponding author
Additional information
Communicated by BJ Rao.
Corresponding editor: BJ Rao
Rights and permissions
About this article
Cite this article
Dave, V., Gupta, A., Singh, P. et al. PEGylated Lipova E120 liposomes loaded with celecoxib: in-vitro characterization and enhanced in-vivo anti-inflammatory effects in rat models. J Biosci 44, 94 (2019). https://doi.org/10.1007/s12038-019-9919-x
Received:
Accepted:
Published:
DOI: https://doi.org/10.1007/s12038-019-9919-x