Abstract
Background: Ophthalmology applies many different ways of delivering effective drugs to eye tissue for the prevention and treatment of diseases of various etiologies. The vast majority of ophthalmologists use traditional instillation of drugs in an eye disease. However, this method has a number of drawbacks, in particular, during instillation of drip forms of drugs, up to 80% of the drug is lost due to withdrawal of its tear fluid and rapid absorption by the mucous membrane of the eyes, which necessitates their frequent instillation to maintain the therapeutic concentration in the eyeball.
Objective: The use of polymeric forms of bio soluble antiviral eye medicinal films of prolonged form in ophthalmic practice would allow introducing the active substance less often while maintaining its therapeutic concentration, reducing the dosage of the drug and the negative effect of frequent instillation.
Methods: A method of obtaining polymeric forms of bio soluble nanostructured ophthalmic medicinal films is based on a composition of water-soluble Na-carboxymethylcellulose (Na-CMC) with a degree of substitution of 0.85 ± 2 and a polymerization degree of 630 ± 20 and a derivative of Nacarboxymethylcellulose containing a chemically bound natural polyphenol-gossypol in an amount of polymerization-630 ± 20 and a derivative of Na-carboxymethylcellulose containing chemically bound natural polyphenol-gossypol in an amount of 0 mole% (sodium salt of 2,3-diethoxy – 6 – O – carboxymethyl- (1 → 4) –β – D – ox glucose – oxy-hydroxyl – 2 – ethyl– (1 → 4) –β – D – ox glucose – diethyl hydroxyl-poly –2 – O – carboxymethyl- (1 → 4) - β - D glucose –2.6 - O –dicarboxymethyl- (1 → 4) –β – D glucose); this is the substance of the antiviral drug “CelAgrip”.
Result: In this work the possibility of regulating the bio scission time and physicochemical parameters of ocular medicinal films has been shown, by varying the degree of substitution and degree of polymerization of sodium carboxymethylcellulose and the pH of their aqueous solutions.
Conclusion: The most promising in terms of the prolongation effect and the absence of an irritating effect and transparency are films, obtained from solutions of the polymer-polymer composition of Na- CMC - a “CelAgrip” substance of a spherical shape with embedded nanoparticles of size 14-52 nm and a pH value of 7.6.
Keywords: Antiviral eye films, sodium carboxymethylcellulose, biosoluble film, “CelAgrip” substance, release kinetics, nanoparticles, therapeutic concentration, prolongation mechanism.
Graphical Abstract
[http://dx.doi.org/10.1097/ICU.0b013e32834cd5a9] [PMID: 22081026]
[http://dx.doi.org/10.1134/S0965545X14030183]