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Novel Long Retentive Posaconazole Ophthalmic Suspension

Received: 20 December 2019     Accepted: 3 January 2020     Published: 14 February 2020
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Abstract

Ophthalmic formulations are not completely available for eliciting therapeutic action because of various reasons such as rapid tear drainage, blinking of eye, lower residence time and lower cul de sac volume. Ophthalmic formulation gets easily drained off due to eye blinking due to low viscosity. Posaconazole is known to have antifungal efficacy as oral route, however ophthalmic efficacy is not studied. The objective of present work was to develop long retentive posaconazole ophthalmic suspension based on polymer platform system of carbopol 974 P and xanthan gum. This synergistic polymer platform was pre-identified by means of experimental design study. Polymer based formulation helps to retain the drug at the site of action for longer duration and does not get washed away due to eye blinking phenomenon. Sterilization is key parameters for ophthalmic formulation. Different methods of sterilization were studied for posaconazole drug as well as polymer mixture and finished product. The developed formulations were characterized for homogeneity, pH, particle size, viscosity, osmolality, rheology study, mucoadhesive strength, contact angle, assay of posaconazole and benzalkonium chloride, degradation product, polymorphic form evaluation, eye irritation test and pharmacodynamic efficacy study. A stable long retentive posaconazole ophthalmic formulation was developed based on principles of quality by design. The developed formulation can be easily manufactured at bigger scale without need of any sophisticated equipment.

Published in Pharmaceutical Science and Technology (Volume 4, Issue 1)
DOI 10.11648/j.pst.20200401.11
Page(s) 1-10
Creative Commons

This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.

Copyright

Copyright © The Author(s), 2020. Published by Science Publishing Group

Keywords

Ocular Long Retentive, Posaconazole, Ophthalmic Suspension

References
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[2] Cholkar K, Dasari SR, Pal D, Mitra AK. Eye: Anatomy, physiology and barriers to drug delivery. In: Mitra AK (ed.). Ocular transporters and receptors: their role in drug delivery. Woodhead Publishing Series in Biomedicine 2012: 1–36.
[3] S. Roy, K. Pal, A. Anis, K. Pramanik & B. Prabhakar (2009) Polymers in Mucoadhesive Drug-Delivery Systems: A Brief Note, Designed Monomers and Polymers, 12: 6, 483-495, DOI: 10.1163/138577209X12478283327236.
[4] Gupta Somya, Parvez Nayyar, Bhandari Akanksha, Sharma Pramod Kumar, Interpenetrating polymer network-based drug delivery systems: emerging applications and recent patents, volume 4, issue 2, 2014, 75-86.
[5] Simta S Jadhav, Millind J Bhitre, Kavita Inamdar, Identification of Polymer Synergy with Help of DOE, International Journal of Emerging Technologies in Engineering Research (IJETER) January 2018, Volume 6, Issue 1.
[6] Lik Thai Lim, Elliott Y. Ah-kee, and Cian E. Collins, Common eye drops and their implications for pH measurements in the management of chemical eye injuries, International Journal of Ophthalmology. 2014; 7 (6): 1067–1068.
[7] Sandle, Tim. Sterile Ophthalmic Preparations and Contamination Control. Journal of GXP Compliance (2014), 18. 1-5.
[8] Chapter 1229, united state pharmacopeia.
[9] Priyanka Patel, Kajal Ahir, Vandana Patel, Lata Manani, Chirag Patel, Drug-Excipient compatibility studies: First step for dosage form development, The Pharma Innovation Journal 2015; 4 (5): 14-20.
[10] Anton Paar GmbH: e-learning course – Basics of Rheometry, part 1: Rotation; part 2: Oscillation. Graz, 2010.
[11] Barnes, H. A., Hutton, J. F., Walters, K.: An introduction to rheology. Elsevier, Amsterdam, 1989. Barnes, H. A.: A handbook of elementary rheology. Inst. of Non-Newt. Fluid Mechanics, Aberystwyth, 2000. Barnes, H. A.: Viscosity. INNFM, Aberystwyth, 2000
[12] Macosko, C. W.: Rheology, principles, measurements, and applications. Wiley, New York, 1994.
[13] Contact angle, www.krussscientific.com.
[14] Malvern Pananalytical, Pharmaceutical Formulations and the Importance of Zeta Potential to Pharmaceutical Formulations, May 12, 2005.
[15] Draize J, Woodward G, Calvery O, Methods for the study of toxicity and irritation of substance applied locally to the skin surface and mucous membrane, Journal of Pharmacology and Experimental Therapeutics, Vol. 82, No. 3, 1944, pp. 377-390.
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  • APA Style

    Jadhav Simta, Inamdar Kavita, Bhitre Milind. (2020). Novel Long Retentive Posaconazole Ophthalmic Suspension. Pharmaceutical Science and Technology, 4(1), 1-10. https://doi.org/10.11648/j.pst.20200401.11

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    ACS Style

    Jadhav Simta; Inamdar Kavita; Bhitre Milind. Novel Long Retentive Posaconazole Ophthalmic Suspension. Pharm. Sci. Technol. 2020, 4(1), 1-10. doi: 10.11648/j.pst.20200401.11

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    AMA Style

    Jadhav Simta, Inamdar Kavita, Bhitre Milind. Novel Long Retentive Posaconazole Ophthalmic Suspension. Pharm Sci Technol. 2020;4(1):1-10. doi: 10.11648/j.pst.20200401.11

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  • @article{10.11648/j.pst.20200401.11,
      author = {Jadhav Simta and Inamdar Kavita and Bhitre Milind},
      title = {Novel Long Retentive Posaconazole Ophthalmic Suspension},
      journal = {Pharmaceutical Science and Technology},
      volume = {4},
      number = {1},
      pages = {1-10},
      doi = {10.11648/j.pst.20200401.11},
      url = {https://doi.org/10.11648/j.pst.20200401.11},
      eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.pst.20200401.11},
      abstract = {Ophthalmic formulations are not completely available for eliciting therapeutic action because of various reasons such as rapid tear drainage, blinking of eye, lower residence time and lower cul de sac volume. Ophthalmic formulation gets easily drained off due to eye blinking due to low viscosity. Posaconazole is known to have antifungal efficacy as oral route, however ophthalmic efficacy is not studied. The objective of present work was to develop long retentive posaconazole ophthalmic suspension based on polymer platform system of carbopol 974 P and xanthan gum. This synergistic polymer platform was pre-identified by means of experimental design study. Polymer based formulation helps to retain the drug at the site of action for longer duration and does not get washed away due to eye blinking phenomenon. Sterilization is key parameters for ophthalmic formulation. Different methods of sterilization were studied for posaconazole drug as well as polymer mixture and finished product. The developed formulations were characterized for homogeneity, pH, particle size, viscosity, osmolality, rheology study, mucoadhesive strength, contact angle, assay of posaconazole and benzalkonium chloride, degradation product, polymorphic form evaluation, eye irritation test and pharmacodynamic efficacy study. A stable long retentive posaconazole ophthalmic formulation was developed based on principles of quality by design. The developed formulation can be easily manufactured at bigger scale without need of any sophisticated equipment.},
     year = {2020}
    }
    

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    AU  - Bhitre Milind
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    DO  - 10.11648/j.pst.20200401.11
    T2  - Pharmaceutical Science and Technology
    JF  - Pharmaceutical Science and Technology
    JO  - Pharmaceutical Science and Technology
    SP  - 1
    EP  - 10
    PB  - Science Publishing Group
    SN  - 2640-4540
    UR  - https://doi.org/10.11648/j.pst.20200401.11
    AB  - Ophthalmic formulations are not completely available for eliciting therapeutic action because of various reasons such as rapid tear drainage, blinking of eye, lower residence time and lower cul de sac volume. Ophthalmic formulation gets easily drained off due to eye blinking due to low viscosity. Posaconazole is known to have antifungal efficacy as oral route, however ophthalmic efficacy is not studied. The objective of present work was to develop long retentive posaconazole ophthalmic suspension based on polymer platform system of carbopol 974 P and xanthan gum. This synergistic polymer platform was pre-identified by means of experimental design study. Polymer based formulation helps to retain the drug at the site of action for longer duration and does not get washed away due to eye blinking phenomenon. Sterilization is key parameters for ophthalmic formulation. Different methods of sterilization were studied for posaconazole drug as well as polymer mixture and finished product. The developed formulations were characterized for homogeneity, pH, particle size, viscosity, osmolality, rheology study, mucoadhesive strength, contact angle, assay of posaconazole and benzalkonium chloride, degradation product, polymorphic form evaluation, eye irritation test and pharmacodynamic efficacy study. A stable long retentive posaconazole ophthalmic formulation was developed based on principles of quality by design. The developed formulation can be easily manufactured at bigger scale without need of any sophisticated equipment.
    VL  - 4
    IS  - 1
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Author Information
  • Department of Pharmaceutical Chemistry, C. U. Shah College of Pharmacy, Mumbai, India

  • Department of Pharmaceutical Chemistry, C. U. Shah College of Pharmacy, Mumbai, India

  • Department of Pharmaceutical Chemistry, C. U. Shah College of Pharmacy, Mumbai, India

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