Multifunctional approach with LHRH-mediated PLGA nanoconjugate for site-specific codelivery of curcumin and BCL2 siRNA in mice lung cancer DOI Creative Commons

Madhuchandra Lahan,

Trideep Saikia, Kalpajit Dutta

и другие.

Future Journal of Pharmaceutical Sciences, Год журнала: 2024, Номер 10(1)

Опубликована: Ноя. 20, 2024

Abstract Background Lung cancer remains a leading type, but current chemotherapy is limited by issues including poor drug delivery, toxicity, and resistance. To address these challenges, we developed novel PLGA-PEG-LHRH (PPL) nanoconjugate system for improved delivery. Curcumin, known its anticancer P-gp inhibition properties, was co-loaded with bcl2siRNA (bclsR) to inhibit the bcl2 protein, thus overcoming both resistance mechanisms. Results The PPL conjugate successfully synthesized characterized using FTIR, 1 H NMR, XRD, XPS BCA assay. Curcumin bclsR-loaded PLGA nanoemulsions were prepared double emulsion solvent evaporation method characterized. optimized had size of 179 ± 16 nm, favorable zeta potential, high entrapment, confirmed via TEM. Controlled release studies indicated 83% within 24 h. In vitro revealed significant cytotoxicity against A549 lung cells, showing IC50 8.24 µg/mL compared 21.26 plain curcumin. Enhanced cellular uptake effective targeting cells observed. Molecular analyses demonstrated downregulation MDR1 Bcl2 RNA protein expression, highlighting nanoconjugates' ability suppress Pharmacokinetic in Wistar rats showed superior plasma concentrations, half-life, AUC versus pure suspension. Biodistribution increased accumulation lungs. vivo efficacy Balb/c mice higher tumor ratios CUR-siRNA NPs (66.89%) CUR-PPL (59.84%) which further TNFα p53 levels blood. Histopathological good healing NP- NP-treated Conclusion From study, it may be concluded that system, loaded curcumin bcsR, can potentially effective, multifunctional targeted approach therapy. Graphical

Язык: Английский

Co-delivery of vinorelbine and rutin by lipid polymer nanoparticles for enhanced liver cancer chemotherapy DOI
Bader B. Alsulays, Md. Khalid Anwer, Faisal Imam

и другие.

Journal of Drug Delivery Science and Technology, Год журнала: 2024, Номер unknown, С. 106490 - 106490

Опубликована: Дек. 1, 2024

Язык: Английский

Процитировано

1

Thermoresponsive biomaterial system of Irinotecan and Curcumin for the treatment of colorectal cancer: In-vitro and in-vivo investigations DOI

Aleena Maryiam,

Sibgha Batool,

Zakir Ali

и другие.

Pharmaceutical Development and Technology, Год журнала: 2024, Номер 30(1), С. 37 - 56

Опубликована: Дек. 27, 2024

This study aims to develop a thermoresponsive biomaterial system of irinotecan (IRT) and curcumin (CUR) nano-transferosomal gel (IRT-CUR-NTG) for targeting colorectal cancer (CRC). The IRT-CUR-NTs were statistically optimized loaded into poloxamer-based thermosensitive gel. Transmission electron microscopy (TEM), Differential scanning calorimetry (DSC) Fourier-transform infrared spectroscopy (FTIR) the performed, whereas pH, gelation time, temperature, mucoadhesive strength IRT-CUR-NTG investigated. In-vitro release anticancer analyses explored using HT29 cells. Additionally, in-vivo pharmacokinetics was investigated followed by histopathological examination analysis. PS, PDI, ZP, %EE IRT CUR found be 136.15 nm, 0.143, -15.5 mV, 95.05% 85.12%, respectively. exhibited spherical shape with no chemical interactions among constituents. Similarly, homogenous suitable rectal administration. manifested prolonged profiles CUR. Moreover, significantly enhanced (4-fold) bioavailability toxicity observed when compared conventional more effective against cell lines. In-vivo antitumor analysis demonstrated reduced tumor volume mass after treatment IRT-CUT-NTG, indicating improved effect. It can concluded that is cancer.

Язык: Английский

Процитировано

1

Multifunctional approach with LHRH-mediated PLGA nanoconjugate for site-specific codelivery of curcumin and BCL2 siRNA in mice lung cancer DOI Creative Commons

Madhuchandra Lahan,

Trideep Saikia, Kalpajit Dutta

и другие.

Future Journal of Pharmaceutical Sciences, Год журнала: 2024, Номер 10(1)

Опубликована: Ноя. 20, 2024

Abstract Background Lung cancer remains a leading type, but current chemotherapy is limited by issues including poor drug delivery, toxicity, and resistance. To address these challenges, we developed novel PLGA-PEG-LHRH (PPL) nanoconjugate system for improved delivery. Curcumin, known its anticancer P-gp inhibition properties, was co-loaded with bcl2siRNA (bclsR) to inhibit the bcl2 protein, thus overcoming both resistance mechanisms. Results The PPL conjugate successfully synthesized characterized using FTIR, 1 H NMR, XRD, XPS BCA assay. Curcumin bclsR-loaded PLGA nanoemulsions were prepared double emulsion solvent evaporation method characterized. optimized had size of 179 ± 16 nm, favorable zeta potential, high entrapment, confirmed via TEM. Controlled release studies indicated 83% within 24 h. In vitro revealed significant cytotoxicity against A549 lung cells, showing IC50 8.24 µg/mL compared 21.26 plain curcumin. Enhanced cellular uptake effective targeting cells observed. Molecular analyses demonstrated downregulation MDR1 Bcl2 RNA protein expression, highlighting nanoconjugates' ability suppress Pharmacokinetic in Wistar rats showed superior plasma concentrations, half-life, AUC versus pure suspension. Biodistribution increased accumulation lungs. vivo efficacy Balb/c mice higher tumor ratios CUR-siRNA NPs (66.89%) CUR-PPL (59.84%) which further TNFα p53 levels blood. Histopathological good healing NP- NP-treated Conclusion From study, it may be concluded that system, loaded curcumin bcsR, can potentially effective, multifunctional targeted approach therapy. Graphical

Язык: Английский

Процитировано

0