Amelioration from the ocular irritant Capsaicin: development and assessment of a Capsazepine in situ gel system for ocular delivery

被引:4
作者
Krishnatreyya, Harshita [1 ,2 ]
Hazarika, Hemanga [1 ]
Saha, Achintya [2 ]
Mandal, Santa [1 ]
Bora, Nilutpal Sharma [1 ]
Kishor, Sumit [1 ]
Bhutia, Yangchen Doma [1 ]
Goyary, Danswrang [1 ]
Karmakar, Sanjeev [1 ]
Chattopadhyay, Pronobesh [1 ]
机构
[1] Def Res & Dev Org DRDO, Def Res Lab DRL, Div Pharmaceut Technol, Tezpur 784001, Assam, India
[2] Univ Calcutta, Dept Chem Technol, Pharmaceut & Fine Chem Div, Kolkata, India
关键词
Capsazepine; capsaicin; ocular; in situ gel; formulation; pharmacology; DRUG-DELIVERY; CHITOSAN; CONSTITUENT; RECEPTOR; DESIGN;
D O I
10.1080/17425247.2020.1754396
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Background: Defense personnel utilize capsaicin-based ocular sprays as non-lethal agents for law implementation during instances of mob violence. This study involves the capsaicin antagonist Capsazepine and the investigation of whether Capsazepine's antagonistic approach can be favorably utilized for defense utilization to block capsaicin-initiated pain and inflammation via the ocular pathway. Research design and methods: Ocular capsazepine in situ gels were prepared with polymers Pluronic F-127 and Chitosan; optimized formulation was quantified in ocular tissues chromatographically and by in vivo live ocular imaging; anti-inflammatory efficacy was determined by eye irritation testing, corneal and retinal imaging, ocular prostaglandin estimation, and by viability and proliferation testing using human ocular cell lines, etc. Results: A physicochemically stable Capsazepine in situ gel was formulated which showed little ocular irritation, considerable transcorneal permeation; was precisely quantified in ocular tissues by gas chromatography and in vivo live ocular imaging; showed anti-inflammatory properties against capsaicin by eye imaging experiments, prostaglandin declination and showed acceptable cytocompatibility when studied using human ocular cell lines. Conclusions: The fabricated in situ Capsazepine gel system might be promising for ocular delivery as it appears a pharmacologically potent and safe development, suitable for utilization in the ocular clinical therapy, provided there is additional research to substantiate it.
引用
收藏
页码:863 / 880
页数:18
相关论文
共 31 条
  • [1] Aiyalu R, 2016, BRAZ J PHARM SCI, V52, P493, DOI [10.1590/S1984-82502016000300015, 10.1590/s1984-82502016000300015]
  • [2] In situ gelling systems based on Pluronic F127/Pluronic F68 formulations for ocular drug delivery
    Al Khateb, Kosai
    Ozhmukhametova, Elvira K.
    Mussin, Marat N.
    Seilkhanov, Serzhan K.
    Rakhypbekov, Tolebai K.
    Lau, Wing Man
    Khutoryanskiy, Vitaliy V.
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 502 (1-2) : 70 - 79
  • [3] The potential of chitosan in ocular drug delivery
    Alonso, MJ
    Sánchez, A
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 2003, 55 (11) : 1451 - 1463
  • [4] [Anonymous], 2012, No. 305: Bioaccumulation in Fish: Aqueous and Dietary Exposure.In OECD Guidelines for Testing of Chemicals
  • [5] [Anonymous], PHARM TOXIC
  • [6] TRPV1 (vanilloid receptor, capsaicin receptor) agonists and antagonists
    Appendino, G
    Muñoz, E
    Fiebich, BL
    [J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 2003, 13 (12) : 1825 - 1837
  • [7] Ocular application of chitosan
    Basaran, Ebru
    Yazan, Yasemin
    [J]. EXPERT OPINION ON DRUG DELIVERY, 2012, 9 (06) : 701 - 712
  • [8] TRPV1: A Target for Rational Drug Design
    Carnevale, Vincenzo
    Rohacs, Tibor
    [J]. PHARMACEUTICALS, 2016, 9 (03)
  • [9] The capsaicin receptor: a heat-activated ion channel in the pain pathway
    Caterina, MJ
    Schumacher, MA
    Tominaga, M
    Rosen, TA
    Levine, JD
    Julius, D
    [J]. NATURE, 1997, 389 (6653) : 816 - 824
  • [10] Protein spray-freeze drying.: Effect of atomization conditions on particle size and stability
    Costantino, HR
    Firouzabadian, L
    Hogeland, K
    Wu, CC
    Beganski, C
    Carrasquillo, KG
    Córdova, M
    Griebenow, K
    Zale, SE
    Tracy, MA
    [J]. PHARMACEUTICAL RESEARCH, 2000, 17 (11) : 1374 - 1383