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Latanoprost + Benzalkonium Chloride

Latanoprost + Benzalkonium Chloride

Buy Latanoprost + Benzalkonium Chloride

The US Food and Drug Administration (FDA) has approved latanoprost ophthalmic emulsion solution (XELPROS) .005% as the first and only benzalkonium chloride-free (BAK-free) form of latanoprost.

The therapy, from Sun Pharmaceutical Industries, received New Drug Application (NDA) approval and indication for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. The NDA was approved based on the results of randomized, controlled clinical trials involving patients with open-angle glaucoma or ocular hypertension, and mean baseline IOP of 23-26 mmHg.

The translucent ophthalmic emulsion lowered patient IOP by a mean 6-8 mmHg from baseline, according to Sun Pharmaceuticals. The most frequently reported adverse reactions to patient eyes across multiple trials were pain/stinging upon administration, and ocular hyperemia (redness). Both events were reported in 55% and 41% of patients administered the solution, respectively. As a result, less than 1% of patients discontinued therapy due to intolerance.

As a prostaglandin analogue that serves as a first-line treatment for its indicated conditions, XELPROS is recommended at doses of 1 drop in each infected eye once daily in the evening. Reduction of IOP is intended to begin 3-4 hours following administration, with maximum effect being observed 8-12 hours following.

Anil Raghavan, chief executive officer of Sun Pharma Advanced Research Company (SPARC), called the approved a significant milestone for the company—one that validates its Swollen Micelle Microemulsion technology used to solubilize drugs in lieu of BAK.

Abhay Gandhi, chief executive officer of North America Sun Pharma, echoed those sentiments for the company’s technology, as well as its Ophthalmics division.

Methods

Cells from a human lens epithelial cell line (SRA01/04) were cultured in Dulbecco minimum essential medium supplemented with 5% fetal bovine serum. The amounts of latanoprost (50 µg/mL), timolol maleate (5 mg/mL), or benzalkonium chloride (200 µg/mL) used in eyedrops, and ×10 to×1000 dilutions thereof, were added to the medium. After 7 days' culture, cell morphological changes were assessed using phase-contrast microscopy, and cell-free culture supernatants were collected for prostaglandin E2 (PGE2), interleukin 1α (IL-1α), and interleukin 6 (IL-6) iodine I 125 radioimmunoassay, enzyme-linked immunosorbent assay, and chemiluminescent enzyme immunoassay, respectively.

Conclusion 

Our results indicate that benzalkonium chloride, used as the preservative in eyedrops containing latanoprost or timolol, is the agent most damaging to lens epithelial cells and most strongly stimulates the expression of soluble chemical mediators in these cells. 

Fluorescein and Rose Bengal Staining

One microliter of 1% fluorescein sodium was instilled in the conjunctival sac and then rinsed with PBS 1 minute later. The eyes were examined and photographed under a slit-lamp microscope with a cobalt blue filter and a digital camera (Topcon, Tokyo, Japan). Five corneal areas were considered, the area of positive corneal staining was scored from 0 (absent) to 3 (diffuse loss of epithelium). 16 

Thirty minutes later, the disappearance of staining was observed under a slit-lamp microscope. One microliter of 1% rose bengal was instilled into the conjunctival sac. Fifteen seconds later, the scores were graded according to the van Bijsterveld grading system under a slit-lamp microscope (Topcon). 17

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