Formulation development and upscaling of lipid nanocapsules as a drug delivery system for a novel cyclic GMP analogue intended for retinal drug deliveryShow others and affiliations
2021 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 602, article id 120640Article in journal (Refereed) Published
Abstract [en]
Lipid nanocapsules (LNCs) were prepared with a novel cyclic GMP analogue, DF003, intended for the treatment of neurodegenerative retinal degenerations. LNCs loaded with DF003 were prepared by a phase inversion method and characterized for particle size, polydispersity index, drug loading, entrapment efficiency, stability, and in vitro drug release. Particle size, PdI and zeta potential of selected optimized formulation were 76 ± 1.2 nm, 0.16 ± 0.02, and −11.6 ± 0.4 mV, respectively, with an entrapment efficiency of 69 ± 0.5%. The selected formulation showed a sustained drug release for up to 6 days in phosphate buffer as well as in vitreous components. Stability evaluation of LNCs in presence of vitreous components demonstrated structural stability and compatibility. Further, the nanoparticle preparation process was upscaled to 1000 times (10 L) of the typical lab scale (0.01 L). Product parameters were observed to be unaffected by the upscaling, demonstrating that the LNCs were of the same quality as those prepared at lab scale. Additionally, the manufacturing process was adapted and assessed for a continuous production of LNCs to leverage it for industrial viability. Overall, these findings reveal the remarkable potential of LNCs as drug delivery vehicles and their possibility for clinical translation.
Place, publisher, year, edition, pages
2021. Vol. 602, article id 120640
Keywords [en]
Lipid nanocapsules, Retinal degenerations, Drug Release, Upscaling, Continuous manufacture, Clinical translation
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:ri:diva-53129DOI: 10.1016/j.ijpharm.2021.120640OAI: oai:DiVA.org:ri-53129DiVA, id: diva2:1556421
2021-05-212021-05-212025-09-23Bibliographically approved