Efficacy Assessment of Celecoxib Oil Drops Versus Arachidonic Acid Stimulated Ophthalmic Inflammation in Rabbits

Sharma, Anil K.1, Sahoo, Prabhat K.1, Sharma, Navneet2, Sharma, Rakesh K.2, Tyagi, Amit2
1Delhi Institute of Pharmaceutical Sciences and Research, Formerly College of Pharmacy, University of Delhi, New Delhi, India
2Division of CBRN Defence, Institute of Nuclear Medicine and Allied Sciences, Delhi, India

Tóm tắt

The most comfortable approach to deliver an active pharmaceutical ingredient to the eye has been via topical instillation of aqueous drops. However, the aqueous drops suffer a major setback due to the rapid drainage leading to loss of drug. The aim of the present work was to formulate oil preparations of celecoxib in different oils. Partition behavior, trans-corneal permeation, viscosity, in vivo anti-inflammatory study and gamma scintigraphy of the preparations were investigated. Incorporation of benzyl alcohol resulted in a significant increase in drug permeation across the cornea (p < 0.05). The in vivo efficacy of optimized castor oil formulation was found to be better than control as well as CXB-aqueous suspensions in arachidonic acid triggered eye swelling model in rabbits. Further, results of gamma scintigraphy also indicated prolonged retention. Therefore, the oil eye drops may be a promising alternative, to aqueous eye drops circumventing poor retention in management of ocular ailments.

Tài liệu tham khảo

citation_journal_title=J Ocul Pharmacol; citation_title=Topical arachidonic acid: a model for screening anti-inflammatory agents; citation_author=MB Abelson, SI Butrus, GH Kliman, DL Larson, EJ Corey, LM Smith; citation_volume=3; citation_publication_date=1987; citation_pages=63-74; citation_doi=10.1089/jop.1987.3.63; citation_id=CR1 citation_journal_title=J Ocul Pharmacol Ther; citation_title=The pathophysiologic role of cyclooxygenases in the eye; citation_author=ZA Radi, JA Render; citation_volume=24; citation_issue=2; citation_publication_date=2008; citation_pages=141-151; citation_doi=10.1089/jop.2007.0078; citation_id=CR2 citation_journal_title=Arch Ophthalmol; citation_title=Topical nonsteroidal agents and corneal wound healing; citation_author=PS Hersh, BA Rice, JC Baer, PA Wells, SE Lynch, LJ McGuigan; citation_volume=108; citation_issue=4; citation_publication_date=1990; citation_pages=577-583; citation_doi=10.1001/archopht.1990.01070060125062; citation_id=CR3 citation_journal_title=Br J Ophthalmol; citation_title=Topical use of indomethacin on the day of cataract surgery; citation_author=AE Searle, JL Pearce, DE Shaw; citation_volume=74; citation_issue=1; citation_publication_date=1990; citation_pages=19-21; citation_doi=10.1136/bjo.74.1.19; citation_id=CR4 citation_journal_title=Arch Ophthalmol; citation_title=Use of flurbiprofen to inhibit corneal neovascularization; citation_author=CA Cooper, MV Bergamini, IH Leopold; citation_volume=98; citation_issue=6; citation_publication_date=1980; citation_pages=1102-1105; citation_doi=10.1001/archopht.1980.01020031092017; citation_id=CR5 citation_journal_title=Indian J Exp Biol; citation_title=In vitro transcorneal permeation of ketorolac tromethamine from buffered and unbuffered aqueous ocular drops; citation_author=M Malhotra, DK Majumdar; citation_volume=35; citation_issue=9; citation_publication_date=1997; citation_pages=941-947; citation_id=CR6 citation_journal_title=Colloids Surf B Biointerfaces; citation_title=Eudragit RL 100-based nanoparticulate system of aceclofenac for ocular delivery; citation_author=R Katara, DK Majumdar; citation_volume=103; citation_publication_date=2013; citation_pages=455-462; citation_doi=10.1016/j.colsurfb.2012.10.056; citation_id=CR7 citation_journal_title=Arch Ophthalmol; citation_title=Inhibition of blood-aqueous humor barrier breakdown with diclofenac. A fluorophotometric study; citation_author=MC Kraff, DR Sanders, L McGuigan, MG Raanan; citation_volume=108; citation_issue=3; citation_publication_date=1990; citation_pages=380-383; citation_doi=10.1001/archopht.1990.01070050078035; citation_id=CR8 citation_journal_title=Proc Natl Acad Sci USA; citation_title=Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: the human pharmacology of a selective inhibitor of COX-2; citation_author=BF McAdam, F Catella-Lawson, IA Mardini, S Kapoor, JA Lawson, GA FitzGerald; citation_volume=96; citation_issue=1; citation_publication_date=1999; citation_pages=272-277; citation_doi=10.1073/pnas.96.1.272; citation_id=CR9 citation_title=Design and evaluation of ophthalmic pharmaceutical products; citation_inbook_title=Modern pharmaceutics; citation_publication_date=1990; citation_pages=539-603; citation_id=CR10; citation_author=G Hecht; citation_author=RE Roehrs; citation_author=ER Cooper; citation_author=JW Hiddemen; citation_author=BF VanDuzee; citation_publisher=Marcel Dekker citation_journal_title=AAPS PharmSciTech; citation_title=Aqueous, oil, and ointment formulations of ketorolac: efficacy against prostaglandin E2-induced ocular inflammation and safety: a technical note; citation_author=M Malhotra, DK Majumdar; citation_volume=7; citation_issue=4; citation_publication_date=2006; citation_pages=96; citation_doi=10.1208/pt070496; citation_id=CR11 citation_journal_title=Pharmazie; citation_title=In vitro permeation characteristics of moxifloxacin from oil drops through excised goat, sheep, buffalo and rabbit corneas; citation_author=PK Pawar, DK Majumdar; citation_volume=62; citation_publication_date=2007; citation_pages=853-857; citation_id=CR12 citation_journal_title=Yakugaku Zasshi; citation_title=In vitro corneal permeation of diclofenac from oil drops; citation_author=M Ahuja, SK Sharma, DK Majumdar; citation_volume=127; citation_issue=10; citation_publication_date=2007; citation_pages=1739-1745; citation_doi=10.1248/yakushi.127.1739; citation_id=CR13 citation_title=Medical laboratory technology: methods and interpretations; citation_publication_date=1999; citation_id=CR14; citation_author=R Sood; citation_publisher=Jaypee Brothers citation_journal_title=J Biol Chem; citation_title=Protein measurement with the Folin phenol reagent; citation_author=OH Lowry, NJ Rosebrough, AL Farr, RJ Randall; citation_volume=193; citation_issue=1; citation_publication_date=1951; citation_pages=265-275; citation_id=CR15 citation_journal_title=AAPS PharmSciTech; citation_title=Albumin microspheres as carriers for the antiarthritic drug celecoxib; citation_author=H Thakkar, RK Sharma, AK Mishra, K Chuttani, RR Murthy; citation_volume=6; citation_issue=1; citation_publication_date=2005; citation_pages=E65-E73; citation_doi=10.1208/pt060112; citation_id=CR16 citation_journal_title=Drug Deliv; citation_title=Fabrication and evaluation of lipid nanoparticulates for ocular delivery of a COX-2 inhibitor; citation_author=AK Sharma, PK Sahoo, DK Majumdar, N Sharma, RK Sharma, A Kumar; citation_volume=23; citation_issue=9; citation_publication_date=2016; citation_pages=3364-3373; citation_doi=10.1080/10717544.2016.1183720; citation_id=CR17 citation_journal_title=Int J Biol Macromol; citation_title=Chitosan nanoparticles amplify the ocular hypotensive effect of cateolol in rabbits; citation_author=null Ameeduzzafar, J Ali, A Bhatnagar, N Kumar, A Ali; citation_volume=65; citation_publication_date=2014; citation_pages=479-491; citation_doi=10.1016/j.ijbiomac.2014.02.002; citation_id=CR18 citation_inbook_title=Remington’s pharmaceutical sciences; citation_publication_date=1990; citation_pages=1687; citation_id=CR19; citation_author=MA Longer; citation_author=JR Robinson; citation_publisher=Mack Publishing Company citation_journal_title=Mediat Inflamm; citation_title=Effect of ricinoleic acid in acute and subchronic experimental models of inflammation; citation_author=C Vieira, S Evangelista, R Cirillo, A Lippi, CA Maggi, S Manzini; citation_volume=9; citation_publication_date=2000; citation_pages=223-228; citation_doi=10.1080/09629350020025737; citation_id=CR20