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Drug Delivery and Translational Research

, Volume 9, Issue 6, pp 1017–1026 | Cite as

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

  • Manish KumarEmail author
  • Pooja Upadhayay
  • Ravi Shankar
  • Monika Joshi
  • Shailendra Bhatt
  • Anuj Malik
Original Article
  • 137 Downloads

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.

Keywords

Chitosan Nanoparticles In situ gel Chlorpheniramine maleate Poloxamer 407 

Notes

Acknowledgments

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

Compliance with ethical standards

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

Conflict of interest

The authors declare that they have no conflict of interest.

Disclaimer

The authors alone are responsible for the content and writing of the paper.

References

  1. 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.CrossRefGoogle Scholar
  2. 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.CrossRefGoogle Scholar
  3. 3.
    Soliman II, Soliman NA, Abdou EM. Formulation and stability study of chlorpheniramine maleate nasal gel. Pharm Dev Technol. 2010;15(5):484–91.CrossRefGoogle Scholar
  4. 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.CrossRefGoogle Scholar
  5. 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.CrossRefGoogle Scholar
  6. 6.
    Arora P, Sharma S, Garg S. Permeability issues in nasal drug delivery. Drug Discov Today. 2002;7:967–75.CrossRefGoogle Scholar
  7. 7.
    Basu S, Bandyopadhyay AK. Nasal drug delivery. AAPS PharmSciTech. 2010;11(3):1223–36.CrossRefGoogle Scholar
  8. 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.CrossRefGoogle Scholar
  9. 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.CrossRefGoogle Scholar
  10. 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. 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.CrossRefGoogle Scholar
  12. 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.CrossRefGoogle Scholar
  13. 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.CrossRefGoogle Scholar
  14. 14.
    Bilirakis D, Papadimitriou S, Avgoustakis K, Karavas E, Georgarakis M. Chitosan nanoparticles loaded with dorzolamide and pramipexole. Carbohydr Polym. 2008;73:44–54.CrossRefGoogle Scholar
  15. 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.CrossRefGoogle Scholar
  16. 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. 17.
    Choi HG, Jung JH, Ryu JM. Development of in situ gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm. 1998;165:33–44.CrossRefGoogle Scholar
  18. 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. 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.Google Scholar
  20. 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.CrossRefGoogle Scholar
  21. 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.CrossRefGoogle Scholar
  22. 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.CrossRefGoogle Scholar
  23. 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.CrossRefGoogle Scholar
  24. 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.CrossRefGoogle Scholar
  25. 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.CrossRefGoogle Scholar
  26. 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.CrossRefGoogle Scholar
  27. 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.CrossRefGoogle Scholar
  28. 28.
    Zhou M, Donovan MD. Intranasal mucociliary clearance of putative bioadhesive polymer gels. Int J Pharm. 1996;135:115–25.CrossRefGoogle Scholar
  29. 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.Google Scholar

Copyright information

© Controlled Release Society 2019

Authors and Affiliations

  1. 1.M M College of PharmacyMaharishi Markandeshwar (Deemed to be University)AmbalaIndia
  2. 2.Department of PharmaceuticsRajiv Academy for PharmacyMathuraIndia
  3. 3.Department of PharmaceuticsSHEAT College of PharmacyVaranasiIndia
  4. 4.Department of PharmaceuticsAshoka Institute of PharmacyVaranasiIndia

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