Cyclosporine A Nanosuspensions for Ophthalmic Delivery: A Comparative Study between Cationic Nanoparticles and Drug-Core Mucus Penetrating Nanoparticles was written by Yan, Rong;Xu, Lai;Wang, Qiuhe;Wu, Zheng;Zhang, Hua;Gan, Li. And the article was included in Molecular Pharmaceutics in 2021.COA of Formula: C25H46ClN The following contents are mentioned in the article:
The effect of mucin on ocular bioavailability depends on the extent to which it acts as a barrier or retention site. Mucus penetrating particles (MPPs) can evade the mucus entrapment and associated rapid clearance, but cationic nanoparticles have high adhesion to the mucosa. Both formulations can prolong the drug residence time on the surface of the eyes. The purpose of this work is to compare the effects of mucoadhesion of cationic nanoparticles and mucous permeability of MPPs on ocular bioavailability. Cationic nanosuspensions and drug-core MPP nanosuspensions were developed using the anti-solvent precipitation method. The results of X-ray diffraction revealed that CsA was amorphous. In vitro mucoadhesion evaluation demonstrated that cationic nanosuspensions enhanced the interaction with pig mucin about 5.0-6.0 fold compared to drug-core MPP nanosuspensions. A mucus permeation study by the transwell diffusion system showed that the Papp values of drug-core MPP nanosuspensions were 5.0-10.0 times higher than those of cationic nanosuspensions. In vivo ocular bioavailability evaluation of those CsA formulations was conducted in rabbits using a conventional nanosuspension as a comparison. The CsA concentrations in the cornea following the administration of a cationic nanosuspension and a drug-core MPP nanosuspension were 13,641.10 ng/g and 11,436.07 ng/g, resp., significantly higher than that of the conventional nanosuspension (8310.762 ng/g). The results showed that both the cationic and MPP nanosuspensions were able to deliver CsA to anterior ocular tissues in effective therapeutic concentrations (10-20μg/g) with topical drop instillation. The cationic nanosuspension could achieve relatively higher bioavailability than the MPP nanosuspension. The cationic nanosuspension would be a promising ocular drug delivery system. This study involved multiple reactions and reactants, such as N-Benzyl-N,N-dimethylhexadecan-1-aminium chloride (cas: 122-18-9COA of Formula: C25H46ClN).
N-Benzyl-N,N-dimethylhexadecan-1-aminium chloride (cas: 122-18-9) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).COA of Formula: C25H46ClN
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics