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Formulation of Polymeric Nanoparticles Loading Baricitinib as a Topical Approach in Ocular Application
Negar Beirampour1, Paola Bustos-Salgado1,2, Núria Garrós1
1Departament de Farmàcia i Tecnologia Farmacèutica, i Fisicoquímica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, Spain.
Pharmaceutics
|August 29, 2024
Summary
This study developed optimized PLGA and PCL nanoparticles for enhanced ocular drug delivery of baricitinib (BTB). These safe and effective nanoparticles improve drug penetration and retention in the eye.
Area of Science:
- Ophthalmology
- Nanotechnology
- Pharmaceutics
Background:
- Topical ocular drug delivery is challenging due to physiological barriers and rapid tear turnover.
- Traditional eye drops have limited efficacy because of poor drug penetration and bioavailability.
- Nanoparticles offer potential advantages for ocular drug delivery, including improved solubility, controlled release, and targeted delivery.
Purpose of the Study:
- To design and optimize poly(lactic-co-glycolic acid) (PLGA) and polycaprolactone (PCL) nanoparticles for ocular delivery of baricitinib (BTB).
- To evaluate the physicochemical properties, microbiological safety, ex vivo permeation, and in vitro ocular tolerance of the developed nanoparticle formulations.
Main Methods:
- Factorial design (2^3+ star design) was employed for nanoparticle optimization.
- Nanoparticle characterization included size, polydispersity index, surface charge, and entrapment efficiency.
- Microbiological safety was assessed using the Challenge Test.
- Ex vivo permeation studies through porcine cornea were conducted.
- In vitro ocular tolerance was evaluated, including HET-CAM testing.
Main Results:
- Optimized PLGA and PCL nanoparticles exhibited small size, low polydispersity, negative surface charge, and high entrapment efficiency.
- The nanoparticle formulations passed the Challenge Test, indicating microbiological safety.
- Ex vivo studies showed a >15-fold increase in baricitinib permeability coefficient compared to a plain solution.
- Nanoparticles demonstrated drug retention and a depot effect in corneal tissue.
- In vitro ocular tolerance studies and HET-CAM testing confirmed no significant irritancy.
Conclusions:
- PLGA and PCL nanoparticles are effective carriers for ocular baricitinib delivery.
- The developed nanoparticles enhance drug permeation and retention within ocular tissues.
- These formulations show promising potential for safe and improved topical ocular drug delivery, minimizing systemic exposure.
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