DOI: 10.21276/ajptr
Fri, 19 Apr 2019

Optimization of the In Vitro Transcorneal Release and the In Vivo IOP-Lowering Effects of Latanoprost Ophthalmic Gel Formulations Using Azone™ as a Penetration Enhancer and Carbopol-974® as a Mucoadhesive

Mohsen. Afouna1*, ashraf Naim2

1.Department of Pharmaceutics & Pharmaceutical Technology, College of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt

2.Department of Pharmacology & Toxicology, College of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia


The objectives of this study were to maximize; a) the in vitro transcorneal release, b) the IOP-lowering effect and, c) the duration of action, of Latanoprost acid (LAT) ophthalmic gels. The in vitro transcorneal release of LAT from a 1st set of gel formulations that containing different concentrations of Azone (as enhancer) with fixed concentration of C-974® (as mucoadhesive) were studied. Formulation that showed greatest permeability parameters at lowest Azone concentration was selected for preparation of a 2nd set of ocular gels containing various C-974® concentrations. The in vitro transcorneal release was assessed, and the best C-974® concentration required for preparation of formulations that can be conceded as ideal ophthalmic LAT gels hve been pinpointed and scaled up for in vivo IOP-lowering efficacy study using TONO-PEN AVIA tonometer in rabbits for 4-consecutive days.  Various test formulations have showed significant but varied augmentations in both, in vitro and in vivo results. Formulations (GAZ-4) & GC-4 have shown the highest therapeutic IOP lowering effects; i.e., (7.8±1.8), (6.5±2.1), respectively. Particularly noteworthy with both formulations the IOP base-line didn’t re-established after 24 hours, and their durations of action in the single-dose study were 47±2.25, and 48±1.5, respectively. The in vitro release, onset, magnitude & duration of action of action of LAT gels have been enhanced and extended for up to 2-day with two gel formulations.  Nonetheless, the success in developing a novel ophthalmic formulation depended for great extent upon the crucial net outcomes of a very sensitive interplay/balance between the drug and additives.

Keywords: Azone; Corneal transport; Ocular delivery; Ocular enhancers; Carbopol-974; Glaucoma; IOP lowering effect; Mucoadhesive

[PDF]   Viewed: 1117   Downloaded: 115
  • Call for paper

    American Journal of PharmTech Research (AJPTR) is a peer-reviewed, bimonthly official international journal allowing access to abstracts and full-text.



  • Email & SMS Alerts

    Email/SMS alert system is one of the key features and gives update information about the submitted manuscript.


  • Article Statastics

    American Journal of PharmTech Research (AJPTR) provides unique facility for authors to know popularity of articles on basis of numbers of PDF download and views. It will display in tabulated format.

  • Online Submission

    American Journal of PharmTech Research (AJPTR) is one of the International open access journal devoted to various disciplines in science and technology.


web counter
web counter