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Chlorpheniramine maleate containing chitosan-based nanoparticle-loaded thermosensitive in situ gel for management in allergic rhinitis

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Abstract

The aim of the present study was to fabricate a thermosensitive gel containing chlorpheniramine maleate (CPM)–loaded nanoparticles following intranasal administration for effective treatment of allergic rhinitis. Chitosan-based nanoparticles were prepared by a precipitation method followed by the addition of developed NPs within the poloxamer 407– and carbopol 934P–based mucoadhesive thermoreversible gel. Developed formulations were evaluated for particle size, PDI, % entrapment efficiency, and % cumulative drug permeation. NP3 formulation was found to be optimized on the basis of minimum particle size (143.9 nm), maximum entrapment efficiency (80.10 ± 0.414%), and highest drug permeation (90.92 ± 0.531%). The optimized formulation NP3 was then formulated into thermoreversible in situ gel. This intensifies the contact between the nasal mucosa and the drug and increases and facilitates the drug absorption which results in increased bioavailability. G4 formulation was selected as the optimized formulation on the basis of gelation ability and mucoadhesive strength. Histology was carried out to examine the damage caused by the optimized G4 formulation. Results revealed no visual signs of tissue damage thus indicated safe nasal delivery of nanoparticulate in situ gel formulation G4. Thus, intranasal CPM NP–loaded in situ gel was found to be a promising formulation for the management of allergic rhinitis.

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References

  1. Taş C, Ozkan Y, Savaşer A, Baykara T. In vitro and ex vivo permeation studies of chlorpheniramine maleate gels prepared by carbomer derivatives. Drug Dev Ind Pharm. 2004;30(6):637–47.

    Article  Google Scholar 

  2. Tas C, Ozkan Y, Savaser A, Baykara T. In vitro release studies of chlorpheniramine maleate from gels prepared by different cellulose derivatives. Farmaco. 2003;58(8):605–11.

    Article  CAS  Google Scholar 

  3. Soliman II, Soliman NA, Abdou EM. Formulation and stability study of chlorpheniramine maleate nasal gel. Pharm Dev Technol. 2010;15(5):484–91.

    Article  CAS  Google Scholar 

  4. Kumar M, Chaturvedi M, Pathak M. A review on mucoadhesive polymer used in nasal drug delivery system. J Adv Pharm Technol Res. 2011;2(4):215–22.

    Article  Google Scholar 

  5. Mishra S, Patel NS, Kumar M, Pathak K. Cross-linked mucoadhesive microspheres based on anionic heteropolysaccharide for nasal delivery of felodipine: optimization and in vitro evaluation. Drug Delivery Letters. 2013;3:136–48.

    Article  CAS  Google Scholar 

  6. Arora P, Sharma S, Garg S. Permeability issues in nasal drug delivery. Drug Discov Today. 2002;7:967–75.

    Article  CAS  Google Scholar 

  7. Basu S, Bandyopadhyay AK. Nasal drug delivery. AAPS PharmSciTech. 2010;11(3):1223–36.

    Article  CAS  Google Scholar 

  8. Wermeling DP, Miller JL, Archer SM, Manaligod JM, Rudy AC. Bioavailability and pharmacokinetics of lorazepam after intranasal, intravenous, and intramuscular administration. J Clin Pharmacol. 2013;41(11):1225–31.

    Article  Google Scholar 

  9. Chu K, Chen L, Xu W, Li H, Zhang Y, Xie W, et al. Preparation of a paeonol-containing temperature-sensitive in situ gel and its preliminary efficacy on allergic rhinitis. Int J Mol Sci. 2013;14:6499–515.

    Article  CAS  Google Scholar 

  10. Schmolka IR. Poloxamers in the pharmaceutical industry. In: Tarcha PJ, editor. Polymers for controlled drug delivery. Boca Raton: CRC Press; 1991. p. 189–214.

    Google Scholar 

  11. Pandurangan DK, Bodagala P, Palanirajan VK, Govindaraj S. Formulation and evaluation of voriconazole ophthalmic solid lipid nanoparticles in situ gel. Int J Pharm Investig. 2016;6(1):56–62.

    Article  CAS  Google Scholar 

  12. El-Gizawy SA, Osman MA, El-Hagaar SM, Hisham DM. Nasal drug delivery of a mucoadhesive oxybutynin chloride gel: in vitro evaluation and in vivo in situ study in experimental rats. Journal of Drug Delivery Science and Technology. 2013;23(6):569–75.

    Article  CAS  Google Scholar 

  13. Nagarwal RC, Kant S, Singh PN, Maiti P, Pandit JK. Polymeric nanoparticulate system: a potential approach for ocular drug delivery. J Control Release. 2009;2 1; 136(1):2–13.

    Article  Google Scholar 

  14. Bilirakis D, Papadimitriou S, Avgoustakis K, Karavas E, Georgarakis M. Chitosan nanoparticles loaded with dorzolamide and pramipexole. Carbohydr Polym. 2008;73:44–54.

    Article  Google Scholar 

  15. Schmolka IR. Artificial skin. I. Preparation and properties of Pluronic F-127 gels for the treatment of burns. J Biomed Mater Res. 1972;6(5):571–82.

    Article  CAS  Google Scholar 

  16. Swamy NGN, Abbas Z. Mucoadhesive in situ gels as nasal drug delivery systems: an overview. Asian J Pharm Sci. 2012;7(3):168–80.

    Google Scholar 

  17. Choi HG, Jung JH, Ryu JM. Development of in situ gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm. 1998;165:33–44.

    Article  CAS  Google Scholar 

  18. Garg A, Garg S, Khar RK. Measurement of bioadhesive strength of mucoadhesive buccal tablet: design of an in vitro assembly. Indian Drugs. 1992;30(8):152–5.

    Google Scholar 

  19. Nisha GS, Maithil P, Charyulu RN. Formulation and development of nasal in situ of Triptans for antimigraine activity. Int J Res Pharm Biomed Sci. 2012;3(2):861–8.

    CAS  Google Scholar 

  20. Majithiya RJ, Ghosh PK, Umrethia ML, Murthy RSR. Thermo reversible-mucoadhesive gel for nasal delivery of sumatriptan. AAPS PharmSciTech. 2006;7(3):E1–7.

    Article  Google Scholar 

  21. Borsali R, Mazzarino L, Travelet C, Murrilo SO, Otsuka I, Paintrand IP, et al. Elaboration of chitosan coated nanoparticles loaded with curcumin for mucoadhesive applications. J Colloid Interface Sci. 2012;370:58–66.

    Article  Google Scholar 

  22. Gan Q, Wang T. Chitosan nanoparticles as protein delivery carrier-systematic examination of fabrication conditions for efficient loading and release. Colloids Surface B. 2007;59:24–34.

    Article  CAS  Google Scholar 

  23. Jayakumar R, Anitha A, Deepagan VG, Divyarani VV, Menon D, Nair SV. Preparation, characterization, in vitro drug release and biological studies of curcumin loaded dextran sulphate-chitosan nanoparticles. Carbohydr Polym. 2011;84:1158–64.

    Article  Google Scholar 

  24. Wang Q, Luo Y, Zhang B, Cheng WH. Preparation, characterization and evaluation of selenite loaded chitosan/tpp nanoparticles with or without zein coating. Carbohydr Polym. 2010;82:942–51.

    Article  Google Scholar 

  25. Bromberg LE, Ron ES. Protein and peptide release from temperature-responsive gels and thermogelling polymer matrices. Adv Drug Deliv Rev. 1998;31:197–221.

    Article  CAS  Google Scholar 

  26. Majithiya RJ, Ghosh PK, Umrethia ML, Murthy RSR. Thermoreversible-mucoadhesive gel for nasal delivery of sumatriptan. AAPS Pharm SciTech. 2006;7(3):E80–6.

    Article  Google Scholar 

  27. Charlton S, Jones NS, Davis SS, Illum L. Distribution and clearance of bioadhesive formulations from the olfactory region in man: effect of polymer type and nasal delivery device. European j biomed pharm Sci. 2007;30:295–302.

    Article  CAS  Google Scholar 

  28. Zhou M, Donovan MD. Intranasal mucociliary clearance of putative bioadhesive polymer gels. Int J Pharm. 1996;135:115–25.

    Article  CAS  Google Scholar 

  29. Jain SA, Chauk DS, Mahajan HS, Tekade AR, Gattani SG. Formulation and evaluation of nasal mucoadhesive microspheres of Sumatriptan succinate. J Microencapsul. 2009;26(8):711-21.

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Acknowledgments

The authors are thankful to Rajiv Academy for Pharmacy, Mathura, for providing the facilities and instruments to carry out this work.

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Authors and Affiliations

  1. M M College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, India

    Manish Kumar, Shailendra Bhatt & Anuj Malik

  2. Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, India

    Pooja Upadhayay

  3. Department of Pharmaceutics, SHEAT College of Pharmacy, Varanasi, India

    Ravi Shankar

  4. Department of Pharmaceutics, Ashoka Institute of Pharmacy, Varanasi, India

    Monika Joshi

Authors
  1. Manish Kumar
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  2. Pooja Upadhayay
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  3. Ravi Shankar
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  4. Monika Joshi
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  5. Shailendra Bhatt
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  6. Anuj Malik
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Correspondence to Manish Kumar.

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For this study, prior clearance from an institutional animal ethics committee (approval number AUHAEC-22/FOP/2014) was obtained.

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Kumar, M., Upadhayay, P., Shankar, R. et al. Chlorpheniramine maleate containing chitosan-based nanoparticle-loaded thermosensitive in situ gel for management in allergic rhinitis. Drug Deliv. and Transl. Res. 9, 1017–1026 (2019). https://doi.org/10.1007/s13346-019-00639-w

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  • DOI: https://doi.org/10.1007/s13346-019-00639-w

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