scholarly journals Tunable Release of Curcumin with an In Silico-Supported Approach from Mixtures of Highly Porous PLGA Microparticles

Materials ◽  
2020 ◽  
Vol 13 (8) ◽  
pp. 1807 ◽  
Author(s):  
Concetta Di Natale ◽  
Valentina Onesto ◽  
Elena Lagreca ◽  
Raffaele Vecchione ◽  
Paolo Antonio Netti
Keyword(s):  
In Silico ◽  
Drug Stability ◽  
Double Emulsion ◽  
Diabetes Therapy ◽  
Vis Spectroscopy ◽  
Tunable Release ◽  
Polymeric Microparticles ◽  
Kinetic Release ◽  
Model Drug ◽  
Drug Pharmacokinetics

In recent years, drug delivery systems have become some of the main topics within the biomedical field. In this scenario, polymeric microparticles (MPs) are often used as carriers to improve drug stability and drug pharmacokinetics in agreement with this kind of treatment. To avoid a mere and time-consuming empirical approach for the optimization of the pharmacokinetics of an MP-based formulation, here, we propose a simple predictive in silico-supported approach. As an example, in this study, we report the ability to predict and tune the release of curcumin (CUR), used as a model drug, from a designed combination of different poly(d,l-lactide-co-glycolide) (PLGA) MPs kinds. In detail, all CUR–PLGA MPs were synthesized by double emulsion technique and their chemical–physical properties were characterized by Mastersizer and scanning electron microscopy (SEM). Moreover, for all the MPs, CUR encapsulation efficiency and kinetic release were investigated through the UV–vis spectroscopy. This approach, based on the combination of in silico and experimental methods, could be a promising platform in several biomedical applications such as vaccinations, cancer-treatment, diabetes therapy and so on.

scholarly journals Drug Release Kinetics of Electrospun PHB Meshes

Materials ◽  
2019 ◽  
Vol 12 (12) ◽  
pp. 1924 ◽  
Author(s):  
Vojtech Kundrat ◽  
Nicole Cernekova ◽  
Adriana Kovalcik ◽  
Vojtech Enev ◽  
Ivana Marova
Keyword(s):  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Toxic Substances ◽  
Antimicrobial Efficiency ◽  
Vis Spectroscopy ◽  
Model Drug ◽  
Phosphate Buffered Saline ◽  
Kinetics Of

Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.

scholarly journals Liposome Consolidated with Cyclodextrin Provides Prolonged Drug Retention Resulting in Increased Drug Bioavailability in Brain

2020 ◽  
Vol 21 (12) ◽  
pp. 4408 ◽  
Author(s):  
En-Yi Lin ◽  
Yu-Shuan Chen ◽  
Yuan-Sheng Li ◽  
Syuan-Rong Chen ◽  
Chia-Hung Lee ◽  
...  
Keyword(s):  
Brain Tumors ◽  
Oral Delivery ◽  
Drug Stability ◽  
Resonance Spectroscopy ◽  
Drug Resistant ◽  
Drug Bioavailability ◽  
Delivery Methods ◽  
Liposomal Formulations ◽  
Transmission Electron ◽  
Vis Spectroscopy

Although butylidenephthalide (BP) is an efficient anticancer drug, its poor bioavailability renders it ineffective for treating drug-resistant brain tumors. However, this problem is overcome through the use of noninvasive delivery systems, including intranasal administration. Herein, the bioavailability, drug stability, and encapsulation efficiency (EE, up to 95%) of BP were improved by using cyclodextrin-encapsulated BP in liposomal formulations (CDD1). The physical properties and EE of the CDD1 system were investigated via dynamic light scattering, transmission electron microscopy, UV–Vis spectroscopy, and nuclear magnetic resonance spectroscopy. The cytotoxicity was examined via MTT assay, and the cellular uptake was observed using fluorescence microscopy. The CDD1 system persisted for over 8 h in tumor cells, which was a considerable improvement in the retention of the BP-containing cyclodextrin or the BP-containing liposomes, thereby indicating a higher BP content in CDD1. Nanoscale CDD1 formulations were administered intranasally to nude mice that had been intracranially implanted with temozolomide-resistant glioblastoma multiforme cells, resulting in increased median survival time. Liquid chromatography–mass spectrometry revealed that drug biodistribution via intranasal delivery increased the accumulation of BP 10-fold compared to oral delivery methods. Therefore, BP/cyclodextrin/liposomal formulations have potential clinical applications for treating drug-resistant brain tumors.

scholarly journals Development of enoxaparin sodium polymeric microparticles for colon-specific delivery

2015 ◽  
Vol 88 (3) ◽  
pp. 357-365 ◽  
Author(s):  
Dana Hales ◽  
Maxime Casteran ◽  
Anne Sapin-Minet ◽  
Ioan Tomuţa ◽  
Marcela Achim ◽  
...  
Keyword(s):  
Organic Phase ◽  
Polymer Concentration ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
Colonic Delivery ◽  
Simulated Environment ◽  
Alginate Concentration ◽  
Polymeric Microparticles ◽  
Inflammatory Bowel ◽  
Formulation Factors

Background and aims. Recent studies have shown that low molecular weight heparins are effective in the treatment of inflammatory bowel disease. Therefore, there is considerable interest in the development of an oral colonic delivery pharmaceutical system allowing targeted release of heparin in the inflamed tissue. The objective of this study was to prepare microparticles for the oral administration and colonic release of enoxaparin and to evaluate the influence of certain formulation factors on their characteristics.Methods. Microparticles were prepared by water/oil/water double emulsion technique followed by solvent evaporation. The influence of several formulation factors on the characteristics of microparticles were evaluated. The formulation factors were alginate concentration in the inner aqueous phase, polymer (Eudragit® FS 30D and Eudragit® RS PO) concentration in the organic phase and ratios between the two polymers. The microparticles were characterized in terms of morphology, size, entrapment efficiency and enoxaparin release.Results. The results showed that increasing sodium alginate percentage reduced the encapsulation efficiency of enoxaparin and accelerated enoxaparin release. Regarding the influence of the two polymers, reducing polymer concentration in the organic phase led to a smaller size of microparticles, a lower entrapment efficiency and an important retardation of enoxaparin release. The formulation prepared with Eudragit® FS 30D limited the release to a maximum of 3% in gastric simulated environment, a specific characteristic of oral systems for colonic delivery, and fulfilled our objective to delay the release.Conclusions. Microparticles prepared with Eudragit® FS 30D represent a suitable and potential oral system for the colonic delivery of enoxaparin.

Novel polydatin-loaded chitosan nanoparticles for safe and efficient type 2 diabetes therapy: In silico, in vitro and in vivo approaches

2020 ◽  
Vol 154 ◽  
pp. 1496-1504 ◽  
Author(s):  
Adel Abdel-Moneim ◽  
Ahmed El-Shahawy ◽  
Ahmed Ismail Yousef ◽  
Sanaa Mahmoud Abd El-Twab ◽  
Zienab Essam Elden ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
In Silico ◽  
Chitosan Nanoparticles ◽  
Diabetes Therapy ◽  
Efficient Type

scholarly journals Optimization of the Transwell® System for Assessing the Dissolution Behavior of Orally Inhaled Drug Products through In Vitro and In Silico Approaches

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1109
Author(s):  
Elham Amini ◽  
Abhinav Kurumaddali ◽  
Sharvari Bhagwat ◽  
Simon M. Berger ◽  
Günther Hochhaus
Keyword(s):  
In Silico ◽  
Mass Effect ◽  
Dissolution Behavior ◽  
Experimental Conditions ◽  
Drug Products ◽  
Starting Point ◽  
Orally Inhaled Drug Products ◽  
Model Drug ◽  
The Impact

The aim of this study was to further evaluate and optimize the Transwell® system for assessing the dissolution behavior of orally inhaled drug products (OIDPs), using fluticasone propionate as a model drug. Sample preparation involved the collection of a relevant inhalable dose fraction through an anatomical mouth/throat model, resulting in a more uniform presentation of drug particles during the subsequent dissolution test. The method differed from previously published procedures by (1) using a 0.4 µm polycarbonate (PC) membrane, (2) stirring the receptor compartment, and (3) placing the drug-containing side of the filter paper face downwards, towards the PC membrane. A model developed in silico, paired with the results of in vitro studies, suggested that a dissolution medium providing a solubility of about 5 µg/mL would be a good starting point for the method’s development, resulting in mean transfer times that were about 10 times longer than those of a solution. Furthermore, the model suggested that larger donor/receptor and sampling volumes (3, 3.3 and 2 mL, respectively) will significantly reduce the so-called “mass effect”. The outcomes of this study shed further light on the impact of experimental conditions on the complex interplay of dissolution and diffusion within a volume-limited system, under non-sink conditions.

Preparation and in-vitro evaluation of β-CD/HA nanocomposite as a potential carrier for hydrophobic drugs

2021 ◽  
pp. 088532822110122
Author(s):  
Esmaeil Salimi ◽  
Mohammad Jafar Molaei
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Chemical Bonding ◽  
Ftir Analysis ◽  
Hydrophobic Compounds ◽  
Vis Spectroscopy ◽  
Insoluble Drugs ◽  
Model Drug ◽  
Xrd Patterns

This study aimed to provide a new drug delivery system for hydrophobic compounds. Dexamethasone (DEX) was employed as a hydrophobic model drug, which incorporated into the network of hydroxyapatite (HA)/Cyclodextrin (β-CD) nanocomposite. Phase analysis, chemical bonding, morphology, and drug release was evaluated using XRD, FTIR, FESEM, and UV-vis spectroscopy, respectively. XRD patterns showed the formation of the crystalline structure and FTIR analysis showed the chemical bonding between organic and inorganic phases. FESEM images accompanied by EDX analysis confirmed the presence of HA nano-flakes. Release of DEX loaded β-CD/HA was measured to be around 4.6% and 18.7% in pH5.3 and pH 7.4, respectively. In conclusion, the prepared system could be a potential pH sensitive carrier for sustainable release of water-insoluble drugs.

scholarly journals Magnetoliposomes Incorporated in Peptide-Based Hydrogels: Towards Development of Magnetolipogels

Nanomaterials ◽  
2020 ◽  
Vol 10 (9) ◽  
pp. 1702 ◽  
Author(s):  
Sérgio R. S. Veloso ◽  
Raquel G. D. Andrade ◽  
Beatriz C. Ribeiro ◽  
André V. F. Fernandes ◽  
A. Rita O. Rodrigues ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Magnetic Nanoparticles ◽  
Drug Stability ◽  
Nile Red ◽  
Local Environment ◽  
Proof Of Concept ◽  
Future Developments ◽  
Model Drug ◽  
Biomedical Interest ◽  
Lipid Probe

A major problem with magnetogels is the encapsulation of hydrophobic drugs. Magnetoliposomes not only provide these domains but also improve drug stability and avert the aggregation of the magnetic nanoparticles. In this work, two magnetoliposome architectures, solid and aqueous, were combined with supramolecular peptide-based hydrogels, which are of biomedical interest owing to their biocompatibility, easy tunability, and wide array of applications. This proof-of-concept was carried out through combination of magnetoliposomes (loaded with the model drug curcumin and the lipid probe Nile Red) with the hydrogels prior to pH triggered gelation, and fluorescence spectroscopy was used to assess the dynamics of the encapsulated molecules. These systems allow for the encapsulation of a wider array of drugs. Further, the local environment of the encapsulated molecules after gelation is unaffected by the used magnetoliposome architecture. This system design is promising for future developments on drug delivery as it provides a means to independently modify the components and adapt and optimize the design according to the required conditions.

Electrospun MWCNTs/Poly(lactic-co-glycolic acid) Composite Nanofibrous Drug Delivery System

2012 ◽  
Vol 424-425 ◽  
pp. 1220-1223 ◽  
Author(s):  
Rui Ling Qi ◽  
Hui Juan Liu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Carriers ◽  
Mouse Fibroblast ◽  
Burst Release ◽  
Vis Spectroscopy ◽  
Multi Walled Carbon Nanotubes ◽  
Model Drug

In this study, nanotubular materials multi-walled carbon nanotubes (MWCNTs) were used to encapsulate a model drug, doxorubicine hydrochloride (DOX). Then, the drug-loaded nanotubes (DOX/CNTs) with an optimized drug encapsulation percentage were mixed with poly (lactide-co-glycolide) (PLGA) polymer solution for subsequent electrospinning to form drug-loaded composite nanofibrous mats. The morphology was characterized using scanning electron microscopy (SEM). The proliferation of mouse fibroblast cells cultured on both PLGA and CNTs-doped PLGA fibrous scaffolds were compared through 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyl tetrazolium bromide (MTT) assay of cell viability and SEM observation of cell morphology. In vitro drug release behavior was examined using UV-vis spectroscopy. We show that the incorporation of CNTs and DOX/CNTs within the nanofibrous mats does not significantly change the morphology of the mats. In addition, our results indicate that this double-container drug delivery system (both PLGA polymer and CNTs are drug carriers) is beneficial to avoid the burst release of the drug. The drug loaded elctrospinning composite nanofibrous mats developed in this study may find various applications in tissues engineering and pharmaceutical sciences.

Sign in / Sign up

Export Citation Format

Share Document