scholarly journals Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

Drug Delivery ◽  
2016 ◽  
Vol 23 (9) ◽  
pp. 3712-3723 ◽  
Author(s):  
Nirav Patel ◽  
Happy Nakrani ◽  
Mihir Raval ◽  
Navin Sheth
Keyword(s):  
Sustained Delivery ◽  
Loteprednol Etabonate ◽  
Ocular Bioavailability

scholarly journals Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 605
Author(s):  
Marie-Emérentienne Cagnon ◽  
Silvio Curia ◽  
Juliette Serindoux ◽  
Jean-Manuel Cros ◽  
Feifei Ng ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Surface Erosion ◽  
Sustained Delivery ◽  
Trimethylene Carbonate ◽  
Poly Ethylene Glycol ◽  
In Situ Forming ◽  
Poly Ethylene ◽  
Long Acting

This article describes the utilization of (methoxy)poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) ((m)PEG–PTMC) diblock and triblock copolymers for the formulation of in situ forming depot long-acting injectables by solvent exchange. The results shown in this manuscript demonstrate that it is possible to achieve long-term drug deliveries from suspension formulations prepared with these copolymers, with release durations up to several months in vitro. The utilization of copolymers with different PEG and PTMC molecular weights affords to modulate the release profile and duration. A pharmacokinetic study in rats with meloxicam confirmed the feasibility of achieving at least 28 days of sustained delivery by using this technology while showing good local tolerability in the subcutaneous environment. The characterization of the depots at the end of the in vivo study suggests that the rapid phase exchange upon administration and the surface erosion of the resulting depots are driving the delivery kinetics from suspension formulations. Due to the widely accepted utilization of meloxicam as an analgesic drug for animal care, the results shown in this article are of special interest for the development of veterinary products aiming at a very long-term sustained delivery of this therapeutic molecule.

Injectable in situ gelling delivery system for the treatment of jawbone infections

2021 ◽  
Author(s):  
Shreshtha Dash ◽  
Somnath Singh ◽  
Alekha K Dash
Keyword(s):  
Lactic Acid ◽  
Sustained Release ◽  
Cell Viability ◽  
Yield Stress ◽  
Delivery System ◽  
Pluronic F127 ◽  
Sustained Delivery ◽  
In Situ Gelling ◽  
Sustained Rate

Aim: A polymeric in situ gelling delivery system for localized and sustained delivery to jawbone infections was developed. Materials & methods: In situ gelling delivery systems were prepared using either poly-dl-lactic acid or chitosan and Pluronic F127/Pluronic F68. Metronidazole nanoparticles were prepared using poly (dl-lactide-co-glycolide) or chitosan. Poly (dl-lactide-co-glycolide) was used for microparticles. Particles were characterized for size, charge and morphology. Results: Viscosity and yield stress of the gels were 0.4 Pa.s and 2 Pa, respectively, with 70% cell viability over 72 h. Around 90% of loaded metronidazole was released at a sustained rate over 1 week. Conclusion: Use of appropriate amount of nano/microparticles in the gel resulted in a sustained release over a period of 1 week – needed for jawbone infection.

scholarly journals An injectable in situ lipid phase transition system for sustained delivery of dabigatran etexilate with low burst release

RSC Advances ◽  
2017 ◽  
Vol 7 (89) ◽  
pp. 56594-56601
Author(s):  
Xuanmiao Zhang ◽  
Mei Hu ◽  
Guangfei Wei ◽  
Mengdi Jia ◽  
Tao Gong ◽  
...  
Keyword(s):  
Phase Transition ◽  
Sustained Release ◽  
Dabigatran Etexilate ◽  
Transition System ◽  
Lipid Phase ◽  
Burst Release ◽  
Sustained Delivery ◽  
Lipid Phase Transition ◽  
Initial Burst

The first report of dabigatran exilate sustained release injection that exhibited great potential in controlling initial burst release.

scholarly journals Sustained Delivery of a Novel Natriuretic Peptide for Three Weeks With In Situ Polymer Precipitation Delivery System

2012 ◽  
Vol 18 (8) ◽  
pp. S63 ◽  
Author(s):  
Soo G. Lim ◽  
Syed Ameenuddin ◽  
John C. Burnett ◽  
Subbu S. Venkatraman ◽  
Horng H. Chen
Keyword(s):  
Natriuretic Peptide ◽  
Delivery System ◽  
Sustained Delivery ◽  
Polymer Precipitation

scholarly journals Balance of Drug Residence and Diffusion in Lacrimal Fluid Determine Ocular Bioavailability in In Situ Gels Incorporating Tranilast Nanoparticles

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1425
Author(s):  
Misa Minami ◽  
Hiroko Otake ◽  
Yosuke Nakazawa ◽  
Norio Okamoto ◽  
Naoki Yamamoto ◽  
...  
Keyword(s):  
Residence Time ◽  
Pluronic F127 ◽  
Lacrimal Fluid ◽  
Significant Difference ◽  
Bead Mill ◽  
Conjunctival Inflammation ◽  
Ocular Bioavailability ◽  
Factor Α ◽  
And Diffusion

We previously designed ophthalmic formulations (nTRA) containing tranilast nanoparticles (Tra-NPs) with high uptake into ocular tissues. In this study, we used in situ gel (ISG) bases comprising combinations of pluronic F127 (F127) and methylcellulose (MC/F127), pluronic F68 (F68/F127), and Carbopol (Car/F127), and we developed in situ gels incorporating Tra-NPs (Tra-NP-incorporated ISNGs) such as nTRA-F127, nTRA-MC/F127, nTRA-F68/F127, and nTRA-Car/F127. Moreover, we demonstrated the therapeutic effect on conjunctival inflammation using lipopolysaccharide-induced rats. Each Tra-NP-incorporated ISNG was prepared by the bead mill method, the particle size was 40–190 nm, and the tranilast release and diffusion from formulation were nTRA > nTRA-F127 > nTRA-F68/F127 > nTRA-Car/F127 > nTRA-MC/F127. In the Tra-NP-incorporated ISNGs, the tranilast residence time in the lacrimal fluid, cornea, and conjunctiva was prolonged, although the Cmax was attenuated in comparison with nTRA. On the other hand, no significant difference in conjunctival inflammation between non- and nTRA-F127-instilled rats was found; however, the nTRA-F68/F127, nTRA-Car/F127, and nTRA-MC/F127 (combination-ISG) attenuated the vessel leakage, nitric oxide, and tumor necrosis factor-α expression. In particular, nTRA-F68/F127 was significant in preventing the conjunctival inflammation. In conclusion, we found that the combination-ISG base prolonged the residence time of Tra-NPs; however, Tra-NP release from the formulation was attenuated, and the Tmax was delayed longer than that in nTRA. The balance of drug residence and diffusion in lacrimal fluid may be important in providing high ocular bioavailability in formulations containing solid nanoparticles.

A pH- and temperature-responsive bioresorbable injectable hydrogel based on polypeptide block copolymers for the sustained delivery of proteins in vivo

2018 ◽  
Vol 6 (3) ◽  
pp. 661-671 ◽  
Author(s):  
Md. Hasan Turabee ◽  
Thavasyappan Thambi ◽  
Huu Thuy Trang Duong ◽  
Ji Hoon Jeong ◽  
Doo Sung Lee
Keyword(s):  
Block Copolymers ◽  
Controlled Delivery ◽  
Sustained Delivery ◽  
Injectable Hydrogel ◽  
Temperature Responsive

A pH- and temperature-responsive in situ-forming injectable hydrogel based on comb-type polypeptide block copolymers for the controlled delivery of proteins has been developed.

Sign in / Sign up

Export Citation Format

Share Document