Formulation and optimisation of bedaquiline nanoemulsions for the potential treatment of multi drug resistant tuberculosis in paediatrics using quality by design DOI Creative Commons

Taiwo Oreoluwa Ajayi,

Madan Poka, Bwalya A. Witika

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Dec. 30, 2024

Bedaquiline is a drug used for the treatment of multidrug-resistant TB in adults and children that currently only commercially available tablet form. The present study was aimed at preparing nanoemulsion (NE) BDQ using natural vegetable oils to deliver BDQ. optimisation surfactant mixtures undertaken Design Experiments (DoE), specifically an optimal mixture design. NEs were optimised while monitoring droplet size (DS), zeta potential (ZP), polydispersity index (PDI) content (DC). further characterised transmission electron microscopy, electrical conductivity, viscosity, pH vitro release studies. NE showed values 191.6 nm ± 2.38 nm, 0.1176 1.69, -25.9 mV 3.00 3.14 0.82 mg/ml DS, PDI, ZP DC respectively. Furthermore, TEM studies demonstrated spherical shape globules. by measuring its viscosity which determined as 53.1 µS/cm, 327 3.05 cP 5.63 1.78, In conclusion, these have great improving solubility, delivery, administration However, are required maximise demonstrate what extent effect against MDR-TB.

Language: Английский

Ex Vivo Biosafety and Efficacy Assessment of Advanced Chlorin e6 Nanoemulsions as a Drug Delivery System for Photodynamic Antitumoral Application DOI Creative Commons
Stéphanie Rochetti do Amaral, Mariza Aires Fernandes,

Felipe Falcão Haddad

et al.

Molecules, Journal Year: 2025, Volume and Issue: 30(3), P. 544 - 544

Published: Jan. 25, 2025

The photosensitizer (PS) in the Photodynamic Therapy (PDT) field represents a key factor, being directly connected to therapeutic efficacy of process. Chlorin e6 is second-generation photosensitizer, approved by FDA with most desired clinical properties for PDT applications, presenting high reactive oxygen species (ROS) generation and proven anticancer properties. However, hydrophobicity major limitation, leading poor biodistribution. To overcome this condition, present work developed an up-to-date nanoemulsion incorporating Ce6 new nanosystem (Ce6/NE). A comprehensive study physicochemical properties, stability, fluorescence characteristics, vitro release profile, vivo ex biocompatibility, was established. nanoemulsions showed particle size stability over six months, no spectroscopic or photophysical alterations. Uptake studies demonstrated internalization Ce6/NE monolayers, biocompatibility at lowest concentrations. HET-CAM assay, however, revealed higher range, also indicating Ce6/NE’s potential cancer treatment through antiangiogenic studies. These findings highlight use promising modulated nanotechnology that promotes low toxicity, bioavailability, site-specific delivery.

Language: Английский

Citations

2
IN SILICO, DEVELOPMENT AND CHARACTERIZATION OF CILNIDIPINE ANALOGUES FOR ENHANCED SOLUBILITY AND THERAPEUTIC POTENTIAL IN THE TREATMENT OF ANGINA PECTORIS DOI Open Access

Pavankumar Krosuri,

M. Mothilal

International Journal of Applied Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown, P. 359 - 375

Published: March 7, 2025

Objective: Angina pectoris remains a significant clinical challenge due to the limitations of current therapies, such as inadequate efficacy and undesirable side effects. This study aims address these issues by developing novel treatment approach based on Cilnidipine analogues nanotechnology, focusing lead compound Analogue (CC5; ZINC101069658). Methods: CC5 was identified most promising candidate its optimal balance lipophilicity, solubility, absorption, synthetic feasibility. A bioinformatics-driven uncovered 60 potential target hub genes related angina pectoris, with Protein-Protein Interaction (PPI) analysis highlighting Estimated Glomerular Filtration Rate (EGFR) key target. Molecular docking Dynamics simulations confirmed stability strong binding affinity EGFR-associated protein (5wb7). SWISSADME revealed moderate poor water low gastrointestinal while HOMO-LUMO studies suggested enhanced chemical stability. The Taguchi design experiments indicated that stirring speed critical for nanoparticle size, stabilizer concentration significantly impacted Encapsulation Efficiency (EE) zeta potential. Results: showed of-8.6 kcal/mol EGFR, pharmacokinetic evaluations favourable absorption supporting CC5’s an optimized therapeutic agent pectoris. nanoparticles exhibited 2.63-fold increase in solubility compared parent compound. Fourier Transform Infrared Spectroscopy, Transmission Electron Microscopy, X-ray Diffraction characterization successful formulation. In vitro dissolution demonstrated superior drug release from CC5-loaded nanoparticulate oral disintegrating tablets, CAF9 (CC5 Formulation 9) showing rapid onset action improved profile (98.89±1.10% at 30 min) controlled (80.58%) marketed preparations (18.85%). Conclusion: demonstrates ZINC101069658, CC5, through reduced Crystallinity. made into Nanoparticles using Pluronic F 188 carrier. These were further formulated tablets good conventional tablets. findings suggest ZINC101069658 could be

Language: Английский

Citations

0
QbD-Employed Formulation and Characterization of Sacubitril-Loaded Solid Lipid Nanoparticles: A Step Forward in Nanotechnology-Based Delivery for Hypertension DOI

Preeti Salve,

Shreyansh Khurpe,

Pranay S. Shirke

et al.

Drug Development and Industrial Pharmacy, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 12

Published: April 23, 2025

To develop and characterize sacubitril-loaded solid lipid nanoparticles (SLNs) using a QbD approach to enhance stability, bioavailability, therapeutic efficacy for improved hypertension management. SAC-loaded SLNs were formulated central composite quadratic model within the framework. Characterization techniques, including transmission electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, confirmed particle morphology, crystallinity, structural integrity. The in vitro antihypertensive activity was evaluated human aortic smooth muscle cells (HASMCs) via MTT assay, assessing cell viability inhibition rates. A novel reverse-phase high-performance liquid chromatography (RP-HPLC) method developed quality control, utilizing C18 column with methanol (80:20 v/v) mobile phase. optimized formulation exhibited size of 184 nm, zeta potential -28 mV, high entrapment efficiency (93.83%), sustained drug release (86.23% over 24 h). In studies demonstrated significant inhibiting hypertension-induced HASMCs, achieving 61.97% rate. Comparative analysis showed superior performance SAC-SLNs standard SAC, highlighting their as an advanced treatment option cardiovascular care RP-HPLC excellent sensitivity (LOD 0.96 µg/mL; LOQ 2.93 µg/mL), linearity (R2 = 0.998), ensuring robust control. are promising platform enhancing SAC delivery improving outcomes, addressing limitations traditional formulations advance therapy critical healthcare.

Language: Английский

Citations

0
Advanced QbD-Based Process Optimization of Clopidogrel Tablets with Insights into Industrial Manufacturing Design DOI Creative Commons

Young Woo Bak,

Mi Ran Woo, Hyuk Jun Cho

et al.

Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(5), P. 659 - 659

Published: May 17, 2025

Background/Objectives: Traditional Quality by Testing (QbT) strategies rely heavily on end-product testing and offer limited insight into how critical process parameters (CPPs) influence product quality. This increases the risk of variability inconsistent outcomes. To overcome these limitations, this study aimed to implement a Design (QbD) approach optimize manufacturing clopidogrel tablets. Methods: A science- risk-based QbD framework was applied identify prioritize key CPPs, intermediate quality attributes (iCQAs), final CQAs across unit operations—pre-blending, dry granulation, post-blending, lubrication, compression. Risk assessment tools statistical design experiments (DoE) were used define proven acceptable ranges (PARs). Results: The revealed strong correlations between CPPs CQAs, allowing definition PARs development robust control strategy. led improved consistency, reduced variability, enhanced understanding. Conclusions: minimized reliance while ensuring high-quality offers novel implementation tailored challenges tablets, providing validated that integrates granulation with process-specific CQAs. These results demonstrate value in achieving pharmaceutical meeting regulatory expectations.

Language: Английский

Citations

0
Exploring nanoparticular platform in delivery of repurposed drug for Alzheimer’s disease: current approaches and future perspectives DOI
Snigdha Chakraborty, Sukriti Vishwas, Vancha Harish

et al.

Expert Opinion on Drug Delivery, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 22

Published: Oct. 13, 2024

Introduction Alzheimer's disease (AD) stands as significant challenge in realm of neurodegenerative disorder. It is characterized by gradual decline cognitive function and memory loss. has already expanded its prevalence to 55 million people worldwide expected rise significantly. Unfortunately, there exists a limited therapeutic option that would mitigate progression. Repurposing existing drugs employing nanoparticle delivery agent presents potential solution address the intricate pathology AD.

Language: Английский

Citations

2
Formulation Design and Evaluation of Ginsenoside Compound K Nanostructured Lipid Carriers Based on Molecular Dynamics Simulations DOI
Wei Shen,

Shili Pan,

Jingying Li

et al.

Journal of Pharmaceutical Innovation, Journal Year: 2024, Volume and Issue: 19(6)

Published: Dec. 1, 2024

Language: Английский

Citations

1
Formulation and optimisation of bedaquiline nanoemulsions for the potential treatment of multi drug resistant tuberculosis in paediatrics using quality by design DOI Creative Commons

Taiwo Oreoluwa Ajayi,

Madan Poka, Bwalya A. Witika

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Dec. 30, 2024

Bedaquiline is a drug used for the treatment of multidrug-resistant TB in adults and children that currently only commercially available tablet form. The present study was aimed at preparing nanoemulsion (NE) BDQ using natural vegetable oils to deliver BDQ. optimisation surfactant mixtures undertaken Design Experiments (DoE), specifically an optimal mixture design. NEs were optimised while monitoring droplet size (DS), zeta potential (ZP), polydispersity index (PDI) content (DC). further characterised transmission electron microscopy, electrical conductivity, viscosity, pH vitro release studies. NE showed values 191.6 nm ± 2.38 nm, 0.1176 1.69, -25.9 mV 3.00 3.14 0.82 mg/ml DS, PDI, ZP DC respectively. Furthermore, TEM studies demonstrated spherical shape globules. by measuring its viscosity which determined as 53.1 µS/cm, 327 3.05 cP 5.63 1.78, In conclusion, these have great improving solubility, delivery, administration However, are required maximise demonstrate what extent effect against MDR-TB.

Language: Английский

Citations

0