Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2023 Aug 14;15(8):2136.
doi: 10.3390/pharmaceutics15082136.

Improving Riparin-A Dissolution through a Laponite Based Nanohybrid

Duanne Mendes Gomes  1 , Lyghia Maria Araújo Meirelles  2   3 , Paulo Monteiro Araujo  1 , Rayran Walter Ramos de Sousa  4 , Paulo Michel Pinheiro Ferreira  4 , Stanley Juan Chavez Gutierrez  1 , Maria das Graças Freire de Medeiros  1 , Fernanda Nervo Raffin  5
Affiliations

Improving Riparin-A Dissolution through a Laponite Based Nanohybrid

Duanne Mendes Gomes et al. Pharmaceutics. .

Abstract

(1) Background: Riparin-A presents several pharmacological activities already elucidated, such as antimicrobial modulator, antileishmania, anxiolytic, anti-inflammatory, antinociceptive, and antioxidant. Even with important bioactive effects, the applicability of Riparin-A is limited due to its low solubility in water, impairing its dissolution in biological fluids. Thus, the objective of this study was to develop a nanohybrid based on Riparin-A and Laponite to obtain a better dissolution profile and evaluate its cytotoxic potential. (2) Methods: The formation of a hybrid system was highlighted by X-ray powder diffraction, infrared spectroscopy, and thermal analysis. Solubility, dissolution, and cytotoxicity studies were performed; (3) Results: An increase in the solubility and aqueous dissolution rate of Riparin-A was observed in the presence of clay. Diffractometric analysis of the hybrid system suggests the amorphization of Riparin-A, and thermal analyses indicated attenuation of decomposition and melting of the Riparin-A after interaction with clay. Furthermore, the nanosystem did not exhibit cytotoxic activity on normal and tumorigenic lines. (4) Conclusions: These results are promising for the development of the Riparin-A/Laponite nanosystem for therapeutic purposes, suggesting an increase in the range of possible routes of administration and bioavailability of this bioactive compound.

Keywords: Laponite; Riparin-A; cytotoxicity; dissolution; nanohybrid.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
UV-Vis spectrophotometric scanning of Rip-A at different concentrations.
Figure 2
Figure 2
Pareto diagram for the effect of the parameters Laponite concentration and stirring time during nanohybrid (Rip-A/Lap) preparation on the Rip-A solubility.
Figure 3
Figure 3
Solubility of Rip-A in the presence of increasing Lap concentrations (0–1.4%, w/v).
Figure 4
Figure 4
TGA/DTG profiles of Rip-A (a), Lap (b), MF (c), and Rip-A/Lap (d).
Figure 5
Figure 5
DSC curve of Rip-A (a), Lap (b), MF (c), and Rip-A/Lap (d).
Figure 6
Figure 6
X-ray powder diffraction pattern of the Rip-A (a), and Lap, MF, and Rip-A/Lap (b).
Figure 7
Figure 7
FTIR spectra of Rip-A (a), Lap (b), MF (c), and nanohybrid Rip-A/Lap (d).
Figure 8
Figure 8
Dissolution curve of free Rip-A and nanohybrid Rip-A/Lap.
Figure 9
Figure 9
In vitro cytotoxic activity of Rip-A, laponite, and nanohybrid on normal and tumor cell lines determined using the MTT assay after 72 h of incubation. * p < 0.05 compared to the vehicle by ANOVA, followed by the Newman–Keuls test.
See this image and copyright information in PMC

References

    1. Balunas M.J., Kinghorn A.D. Drug Discovery from Medicinal Plants. Life Sci. 2005;78:431–441. doi: 10.1016/j.lfs.2005.09.012. - DOI - PubMed
    1. Barbosa Filho J.M., Silva E.C., Bhattacharyya J. Synthesis of Several New Phenylethylamides of Substituted Benzoic Acids. Quim. Nova. 1990;13:332–334.
    1. Nunes G.B.L., Policarpo P.R., Costa L.M., da Silva T.G., Militão G.C.G., Câmara C.A., Barbosa Filho J.M., Gutierrez S.J.C., Islam M.T., de Freitas R.M. In Vitro Antioxidant and Cytotoxic Activity of Some Synthetic Riparin-Derived Compounds. Molecules. 2014;19:4595–4607. doi: 10.3390/molecules19044595. - DOI - PMC - PubMed
    1. Barbosa C.R.d.S., Bezerra A.H., Bezerra S.R., Macêdo N.S., Oliveira-Tintino C.D.d.M., Costa J.G.M.d., Coutinho H.D.M., dos Santos H.S., Cunha F.A.B. da Bioactivities of Isolated and Synthetic Riparins of Aniba Riparia (NEES) MEZ (LAURACEAE): A Brief Review. Phytochem. Lett. 2022;52:149–160. doi: 10.1016/j.phytol.2022.10.009. - DOI
    1. Costa L.M., Macedo E.V., Oliveira F.A.A., Ferreira J.H.L., Gutierrez S.J.C., Peláez W.J., Lima F.C.A., de Siqueira Júnior J.P., Coutinho H.D.M., Kaatz G.W., et al. Inhibition of the NorA Efflux Pump of Staphylococcus Aureus by Synthetic Riparins. J. Appl. Microbiol. 2016;121:1312–1322. doi: 10.1111/jam.13258. - DOI - PubMed

LinkOut - more resources