Development, Characterization and In Vitro Evaluation of Paclitaxel and Anastrozole Co-Loaded Liposome

Vu, Minh Thanh; Nguyen, Dinh Tien Dung; Nguyen, Ngoc Hoi; Le, Van Thu; Dao, The Nam; Nguyen, Thi Hương; Cong, Tien Dung; Pham, Truc Le-Buu; Lam, Tri Duc

doi:10.3390/pr8091110

Cited by 8 publications

(3 citation statements)

References 43 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Where EE % is the % of entrapment efficiency, Mt is total quantity of ANA added, and Mf is the free quantity of the ANA that passes through the ultra-filter of Amicon (unentrapped drug) (9) . Dissolution profiles of anastrozole from polymeric nanoparticles were investigated.…”

Section: Anastrozole Polymeric Nanoparticle Preparation and Character...mentioning

confidence: 99%

Anastrozole Nanoparticles for Transdermal Delivery through Microneedles: Preparation and Evaluation

2022

pnr

View full text Add to dashboard Cite

This study examined transdermal anastrozole (ANA) as an oral alternative. ANA is a nonsteroidal aromatase inhibitor licensed to treat breast cancer and metastatic disease. Estrogen makes breast cancer worse. However, ANA is only available as a once-daily oral tablet. In this work, dissolving microneedles that were loaded with ANA polymeric nanoparticles allowed for the transdermal distribution of anastrozole. Method: ANA polymeric nanoparticles were created by the nanoprecipitation process utilizing the polymeric matrix kollicoat MAE100-55, and their physical characteristics and in-vitro release were investigated. Using different water-soluble polymers and the micro-molding method, four formulas of dissolving microneedles loaded with ANA polymeric nanoparticles were created. Additionally, the prepared needles' morphology, mechanical strength, moisture uptake percentage, and moisture loss percentage were examined. Result: The ANA polymeric nanoparticles are 50.49±7.9nm in size, have a polydispersity index of 0.19±0.07, and have an entrapment efficiency of 75±4.5%. While employing poloxamer188 as a stabilizer, complete drug release took place in 3.5 hours. Among the various polymers used to make dissolving microneedle formulas, M-2 made from PVA demonstrated superior mechanical strength, moisture loss percentage, and moisture uptake. Ex vivo permeation through abdominal rat skin confirmed the penetration-enhancing impact of microneedles as permeation increased by 4.9 times compared to bare skin. Histology found no inflammatory reactions or cellular pathology with needle penetration. Conclusion: It was possible to successfully manufacture polymeric nanoparticles of ANA and load them onto dissolving microneedles with sufficient mechanical strength to penetrate the stratum corneum and permit nanoparticle transdermal delivery.

show abstract

Section: Anastrozole Polymeric Nanoparticle Preparation and Character...mentioning

confidence: 99%

Anastrozole Nanoparticles for Transdermal Delivery through Microneedles: Preparation and Evaluation

2022

pnr

View full text Add to dashboard Cite

show abstract

“…Lipid recovery was estimated by Stewart assay [ 28 ]. Encapsulation efficiency (EE%) and drug-to-lipid mass ratio (D/L, μg/μg) were calculated as described previously [ 29 ].…”

Section: Methodsmentioning

confidence: 99%

Raman Spectroscopy Characterization of Multi-Functionalized Liposomes as Drug-Delivery Systems for Neurological Disorders

et al. 2023

View full text Add to dashboard Cite

The characterization of nanoparticle-based drug-delivery systems represents a crucial step in achieving a comprehensive overview of their physical, chemical, and biological features and evaluating their efficacy and safety in biological systems. We propose Raman Spectroscopy (RS) for the characterization of liposomes (LPs) to be tested for the control of neuroinflammation and microglial dysfunctions in Glioblastoma multiforme and Alzheimer’s disease. Drug-loaded LPs were functionalized to cross the blood–brain barrier and to guarantee localized and controlled drug release. The Raman spectra of each LP component were used to evaluate their contribution in the LP Raman fingerprint. Raman data analysis made it possible to statistically discriminate LPs with different functionalization patterns, showing that each molecular component has an influence in the Raman spectrum of the final LP formulation. Moreover, CLS analysis on Raman data revealed a good level of synthetic reproducibility of the formulations and confirmed their stability within one month from their synthesis, demonstrating the ability of the technique to evaluate the efficacy of LP synthesis using small amount of sample. RS represents a valuable tool for a fast, sensitive and label free biochemical characterization of LPs that could be used for quality control of nanoparticle-based therapeutics.

show abstract

“…Lipid recovery was estimated by Stewart assay [ 24 ]. The encapsulation efficiency (EE%) and drug-to-lipid mass ratio (D/L, μg/μg) were calculated as described [ 25 ]. After purification, sample solutions were adjusted to pH 7.0 by adding PBS and stored at 4 °C until use.…”

Section: Methodsmentioning

confidence: 99%

Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics

Taiarol

Bigogno²,

Sesana

et al. 2022

Cancers

View full text Add to dashboard Cite

Glioblastoma is the most common and aggressive brain tumor, associated with poor prognosis and survival, representing a challenging medical issue for neurooncologists. Dysregulation of histone-modifying enzymes (HDACs) is commonly identified in many tumors and has been linked to cancer proliferation, changes in metabolism, and drug resistance. These findings led to the development of HDAC inhibitors, which are limited by their narrow therapeutic index. In this work, we provide the proof of concept for a delivery system that can improve the in vivo half-life and increase the brain delivery of Givinostat, a pan-HDAC inhibitor. Here, 150-nm-sized liposomes composed of cholesterol and sphingomyelin with or without surface decoration with mApoE peptide, inhibited human glioblastoma cell growth in 2D and 3D models by inducing a time- and dose-dependent reduction in cell viability, reduction in the receptors involved in cholesterol metabolism (from −25% to −75% of protein levels), and reduction in HDAC activity (−25% within 30 min). In addition, liposome-Givinostat formulations showed a 2.5-fold increase in the drug half-life in the bloodstream and a 6-fold increase in the amount of drug entering the brain in healthy mice, without any signs of overt toxicity. These features make liposomes loaded with Givinostat valuable as potential candidates for glioblastoma therapy.

show abstract

Development, Characterization and In Vitro Evaluation of Paclitaxel and Anastrozole Co-Loaded Liposome

Cited by 8 publications

References 43 publications

Anastrozole Nanoparticles for Transdermal Delivery through Microneedles: Preparation and Evaluation

Anastrozole Nanoparticles for Transdermal Delivery through Microneedles: Preparation and Evaluation

Raman Spectroscopy Characterization of Multi-Functionalized Liposomes as Drug-Delivery Systems for Neurological Disorders

Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics

Contact Info

Product

Resources

About