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Novel biocompatible polymer-modified liposome nanoparticles for biomedical applications

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Abstract

The incidence of pulmonary arterial hypertension (PAH) has significantly increased in the past few decades and therefore requires immediate attention. The applications of drug-loaded nano-systems have shown considerable improvements in controlling PAH compared to plain drugs. The purpose of this current investigation was to prepare and characterize sildenafil-encapsulated polyethylene glycol (PEGylated) liposomes for effective treatment of pulmonary arterial hypertension. Liposomes were prepared using thin film hydration method by varying the concentrations of sildenafil, Phospholipon 90-G, cholesterol, mPEG-DSPE2000 to optimize the formulation. The optimized liposomal formulation had mean hydrodynamic diameter, polydispersity index (PDI), zeta potential (ZP) and %EE of 155.3 ± 3.2 nm, 0.19 ± 0.1, − 42.2 ± 0.3 mV and 75.89 ± 0.5%. Transmission electron microscopy (TEM) revealed that liposomes were spherical and homogenously dispersed. FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) confirmed that there was no covalent interaction between the drug and excipients. The release of sildenafil from PEGylated liposomes was found to be sustained compared to free drug. Ex vivo study in the rats showed improved vasorelaxant response for sildenafil loaded liposomes (132. 7 ± 0.7%) compared to pure sildenafil (108.2 ± 0.06%) and marketed Revatio® (113.2 ± 0.8%). In summary, sildenafil loaded PEGylated liposomes produced an impressive vasorelaxant response in rat aortic stip assay and require validation to bring the formulation available for clinical studies in the management of PAH.

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References

  1. Galiè N et al (2015) Initial use of ambrisentan plus tadalafil in pulmonary arterial hypertension. N Engl J Med 373(9):834–844

    Article  PubMed  Google Scholar 

  2. Licarete E, Sesarman A, Banciu M (2015) Exploitation of pleiotropic actions of statins by using tumour-targeted delivery systems. J Microencapsul 32:619–631

    Article  CAS  PubMed  Google Scholar 

  3. Thenappan T et al (2007) A USA-based registry for pulmonary arterial hypertension: 1982–2006. Eur Respir J 30(6):1103–1110

    Article  CAS  PubMed  Google Scholar 

  4. Chin KM et al (2018) psychometric validation of the pulmonary arterial hypertension-symptoms and impact (PAH-SYMPACT) questionnaire: results of the SYMPHONY trial. Chest 154(4):848–861

    Article  PubMed  Google Scholar 

  5. Lau EM et al (2017) Epidemiology and treatment of pulmonary arterial hypertension. Nat Rev Cardiol 14(10):603

    Article  CAS  PubMed  Google Scholar 

  6. Pramanik N et al (2019) Polyhydroxybutyrate-co-hydroxyvalerate copolymer modified graphite oxide based 3D scaffold for tissue engineering application. Mater Sci Eng C 94:534–546

    Article  CAS  Google Scholar 

  7. Segura-Ibarra V et al (2018) Nanotherapeutics for treatment of pulmonary arterial hypertension. Front Physiol 9:890

    Article  PubMed  PubMed Central  Google Scholar 

  8. Nahar K et al (2014) Peptide-coated liposomal fasudil enhances site specific vasodilation in pulmonary arterial hypertension. Mol Pharm 11(12):4374–4384

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  9. Chen L et al (2011) Nanoparticle-mediated delivery of pitavastatin into lungs ameliorates the development and induces regression of monocrotaline-induced pulmonary artery hypertension. Hypertension 57(2):343–350

    Article  CAS  PubMed  Google Scholar 

  10. Rafati N, Caldera F, Trotta F, Ghias N (2019) Pyromellitic dianhydride crosslinked cyclodextrin nanosponges for curcumin controlled release; formulation, physicochemical characterization and cytotoxicity investigations. J Microencapsul. https://doi.org/10.1080/02652048.2019.1669728

    Article  PubMed  Google Scholar 

  11. Shavi GV et al (2016) PEGylated liposomes of anastrozole for long-term treatment of breast cancer: in vitro and in vivo evaluation. J Liposome Res 26(1):28–46

    Article  CAS  PubMed  Google Scholar 

  12. Klibanov AL et al (1990) Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes. FEBS Lett 268(1):235–237

    Article  CAS  PubMed  Google Scholar 

  13. Musteata FM, Pawliszyn J (2006) Determination of free concentration of paclitaxel in liposome formulations. J Pharm Pharm Sci 9:231–237

    CAS  Google Scholar 

  14. Sudhakar B, Krishna MC, Murthy KVR (2016) Factorial design studies of antiretroviral drug-loaded stealth liposomal injectable: PEGylation, lyophilization and pharmacokinetic studies. Appl Nanosci 6(1):43–60

    Article  CAS  Google Scholar 

  15. Yang X et al (2009) A novel liposomal formulation of flavopiridol. Int J Pharm 365(1–2):170–174

    Article  CAS  PubMed  Google Scholar 

  16. Dave V et al (2017) Hybrid nanoparticles for the topical delivery of norfloxacin for the effective treatment of bacterial infection produced after burn. J Microencapsul 34(4):351–365

    Article  CAS  PubMed  Google Scholar 

  17. Shah SP, Misra A (2004) Liposomal amikacin dry powder inhaler: effect of fines on in vitro performance. AAPS PharmSciTech 5(4):107–113

    Article  PubMed Central  Google Scholar 

  18. Lum W et al (2017) Novel liposome-based surface-enhanced raman spectroscopy (SERS) substrate. J Phys Chem Lett 8(12):2639–2646

    Article  CAS  PubMed  Google Scholar 

  19. Biltonen RL, Lichtenberg D (1993) The use of differential scanning calorimetry as a tool to characterize liposome preparations. Chem Phys Lipid 64(1–3):129–142

    Article  CAS  Google Scholar 

  20. Dave V et al (2017) Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis. Appl Nanosci 7(8):973–987

    Article  CAS  Google Scholar 

  21. Korsmeyer RW et al (1983) Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 15(1):25–35

    Article  CAS  Google Scholar 

  22. Tripathi N et al (2018) Discovery of novel soluble epoxide hydrolase inhibitors as potent vasodilators. Sci Rep 8(1):1–11

    Article  Google Scholar 

  23. Mojzych M et al (2016) Relaxant effects of selected sildenafil analogues in the rat aorta. J Enzyme Inhib Med Chem 31(3):381–388

    CAS  PubMed  Google Scholar 

Download references

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Authors and Affiliations

  1. Department of Pharmacy, Banasthali Vidyapith, Tonk, Rajasthan, India

    Sarvesh Paliwal, Jaiprakash Sharma, Vivek Dave, Swapnil Sharma, Kanika Verma, Kajal Tak & Veera Sadhu

  2. Department of Pharmacy, School of Health Science, Central University of South Bihar, Gaya, India

    Vivek Dave

  3. Department of Pharmacy, SMS Medical College, Jaipur, Rajasthan, India

    Jaiprakash Sharma

  4. School of Chemical and Biomolecular Engineering, The University of Sydney, Sydney, NSW, 2006, Australia

    Raghava Reddy Kakarla & Pavan Walvekar

  5. Sonia College of Pharmacy, Dharwad, Karnataka, 580002, India

    Tejraj M. Aminabhavi

Authors
  1. Sarvesh Paliwal
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  2. Jaiprakash Sharma
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  4. Swapnil Sharma
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  5. Kanika Verma
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  6. Kajal Tak
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  7. Raghava Reddy Kakarla
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  8. Veera Sadhu
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  9. Pavan Walvekar
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  10. Tejraj M. Aminabhavi
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Correspondence to Vivek Dave, Raghava Reddy Kakarla or Tejraj M. Aminabhavi.

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Paliwal, S., Sharma, J., Dave, V. et al. Novel biocompatible polymer-modified liposome nanoparticles for biomedical applications. Polym. Bull. 81, 535–547 (2024). https://doi.org/10.1007/s00289-023-04731-7

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  • DOI: https://doi.org/10.1007/s00289-023-04731-7

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