Development and assessment of rhodamine B-loaded nanostructured lipid carrier-based in situ gel for enhanced brain targeting
DOI:
https://doi.org/10.60988/p.v37i2S.243Keywords:
BBB; in situ gel; in vivo; NLC; rhodamine BAbstract
The development of effective drug delivery systems for brain targeting remains a significant challenge due to the restrictive nature of the blood-brain barrier. The intranasal route has emerged as a promising alternative, enabling direct drug transport to brain tissue via the nasal cavity. The primary objective of the present study was to investigate the incorporation of rhodamine B (a model fluorescent marker) into in situ gel-based nanostructured lipid carriers (NLCs) for potential brain targeting via the trigeminal or olfactory pathways. The formulated NLCs were characterized for particle size and polydispersity index (PDI). In vivo biodistribution studies were conducted in rats, which were divided into a control group and a treatment group receiving a single intranasal administration of rhodamine B-loaded NLC in situ gel. The distribution of the nanocarriers within brain tissues was assessed using fluorescence microscopy. The optimized formulation exhibited a mean particle size of 109.3 ± 9.8 nm and a PDI of 0.35 ± 0.07. Biodistribution analysis revealed a time-dependent accumulation of rhodamine B within brain tissues, with peak fluorescence intensity observed at 2 h post-administration. These findings suggest that rhodamine B-loaded NLC in situ gel enhances brain-targeting efficiency and may serve as a viable strategy for intranasal delivery of therapeutics intended for the management of central nervous system disorders.
References
1. Patharapankal E.J., Ajiboye A.L., Mattern C., Trivedi V. Nose-to-brain (N2B) delivery: an alternative route for the delivery of biologics in the management and treatment of central nervous system disorders. Pharmaceutics 16(1), 66, 2023. DOI: 10.3390/pharmaceutics16010066
2. Jaber S.A., Rajab N.A. Preparation and in vitro / ex vivo evaluation of nanoemulsion-based in situ gel for intranasal delivery of lasmiditan. Iraqi J. Pharm. Sci. 33(3), 128–141, 2024. DOI: 10.31351/vol33iss3pp128-141
3. Alkufi H.K., Kassab H.J. Soluplus-stabilized nimodipine-entrapped spanlastic formulations prepared with edge activator (Tween20): comparative physicochemical evaluation. Pharm. Nanotechnol. 13(3), 551–563, 2025. DOI: 10.2174/0122117385348551241028102256
4. Tamer M.A., Kassab H.J. The development of a brain targeted mucoadhesive amisulpride loaded nanostructured lipid carrier. Farmacia 71(5), 1032–1044, 2023. DOI: 10.31925/farmacia.2023.5.18
5. Sabry S.A., Abd El Razek A.M., Nabil M., Khedr S.M., El-Nahas H.M., Eissa N.G. Brain-targeted delivery of Valsartan using solid lipid nanoparticles labeled with rhodamine B; a promising technique for mitigating the negative effects of stroke. Drug Deliv. 30(1), 2179127, 2023. DOI: 10.1080/10717544.2023.2179127
6. Hashim A.A., Rajab N.A. Anastrozole loaded nanostructured lipid carriers: preparation and evaluation. Iraqi J. Pharm. Sci. 30(2), 185–195, 2021. DOI: 10.31351/vol30iss2pp185-195
7. Reimold I., Domke D., Bender J., Seyfried C.A., Radunz H.E., Fricker G. Delivery of nanoparticles to the brain detected by fluorescence microscopy. Eur. J. Pharm. Biopharm. 70(2), 627–632, 2008. DOI: 10.1016/j.ejpb.2008.05.007
8. Tamer M.A., Kassab H.J.. Optimizing intranasal amisulpride loaded nanostructured lipid carriers: formulation, development, and characterization parameters. Pharm. Nanotechnol. 13(2), 287–302, 2025. DOI: 10.2174/0122117385301604240226111533
9. Taher S.S., Al-Kinani K.K. Current nanotechnological strategies for delivery of anti-retroviral drugs: overview and future prospects. Curr. Drug Ther. (in press). DOI: 10.2174/0115748855331460241017100207
10. Bonaccorso A., Musumeci T., Serapide M.F., Pellitteri R., Uchegbu I.F., Puglisi G. Nose to brain delivery in rats: effect of surface charge of rhodamine B labeled nanocarriers on brain subregion localization. Colloids Surf. B Biointerfaces 154, 297–306, 2017. DOI: 10.1016/j.colsurfb.2017.03.035