Engineering of polymer–surfactant nanoparticles of doxycycline hydrochloride for ocular drug delivery

Abstract

Context: Physiologic barriers of the eye, short precorneal drug residence time and poor corneal penetration are the few reasons for reduced ocular bioavailability. Objective: This study was aimed to develop novel polymer-surfactant nanoparticles of hydrophilic drug doxycycline hydrochloride (DXY) to improve precorneal residence time and drug penetration. Materials and methods: Nanoparticles were formulated using emulsion cross-linking method and the formulation was optimized using factorial design. The prepared formulation was characterized for particle size, potential, encapsulation efficiency, in vitro drug release and ex vivo drug diffusion studies. The antibacterial activity studies were also carried out against Escherichia coli and Staphylococcus aureus using the cup-plate method. In vivo eye irritation study was carried out by a modified Draize test in rabbits. Results and discussion: The particle size was found to be in the range of 331-850 nm. About 45-80% of the drug was found to be encapsulated in the nanoparticles. In vitro release demonstrated sustained release profile. Lower flux values in case of nanoparticles as compared to DXY pure drug solution in ex vivo diffusion studies confirmed the sustained release. The nanoparticles were found to be significantly effective (p50.001) than DXY aqueous solution due to sustained release of doxycycline from nanoparticles in both the E. coli and S. aureus strains. The formulation was found to be stable over entire stability period. Conclusion: The developed formulation is safe and suitable for sustained ocular drug delivery.

Ophthalmic Drug Delivery Systems for Antibiotherapy—A Review

“…Ex-vivo studies showed a higher sustained release from particles in both Staphylococcus aureus and Escherichia coli strains than the doxycycline hyclate aqueous solution. The authors noticed that formulations were non-irritating for the eye, inhibited bacterial growth and were a potential drug delivery system for ocular bacterial infections [ 153 ].…”

Approaches in Topical Ocular Drug Delivery and Developments in the Use of Contact Lenses As drug-delivery Devices

“…The nanoparticles (331-850 nm size range) encapsulated around 45-80% of DOX HC. This formulation showed sustained release kinetic of DOX HC with significant antibacterial effect on strains of Staphylococcus aureus and Escherichia coli (p<0.011) as compared to DOX HC aqueous solution [3] .…”

“…The arena of ODD is constantly evolving with potential to exploit the emerging recognition of nano-engineering and polymer science. Over recent years, there has been emphasis on novel, non-evasive delivery devices for not only controlled and sustained ODD but also with applications extended to systemic delivery and theranostics [3][4][5][6][7] , all showing promising results with the potential development of new ocular products in the near future.…”

Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs

“…The designed SPTSs was based on GMO. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) as hydrophilic and hydrophobic model drug were selected for two SPTS@hard capsules, respectively (Pokharkar et al, 2015;Chaturvedi et al, 2017). Appropriate additives were utilized in the two SPTSs, that is, gelucire39/01, PEG 1000 and Tween 80 to adjust their MP and release profiles.…”