Macrophage escape by cholesterol-polyoxyethylene sorbitol oleate micelles for pulmonary delivery

Nanomedicine ◽  
2020 ◽  
Vol 15 (5) ◽  
pp. 489-509
Author(s):  
Dong Shen ◽  
Yan Shen ◽  
Qian Chen ◽  
Bin Huang ◽  
Yedong Mi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Ultrasonic Method ◽  
Pulmonary Delivery ◽  
Single Factor ◽  
Box Behnken Design ◽  
Single Factor Experiment

Aim: Micelles are one of the most promising nanoplatforms for drug delivery, and here, cholesterol-conjugated polyoxyethylene sorbitol oleate (CPSO) micelles have been fabricated for the pulmonary delivery of paclitaxel (PTX). Materials & methods: PTX-CPSO micelles were prepared by a dialysis-ultrasonic method, and a single-factor experiment with a Box–Behnken design was conducted to optimize the formulation. Furthermore, intracellular and phagocytosis escape studies of the optimized formulation were performed on A549 and NR8383 cells. Results: The optimal micelles exhibited satisfactory encapsulation efficiency (78.48 ± 2.36%) and drug loading (17.06 ± 1.71%). In vitro studies showed enhanced CPSO micelle A549 cellular uptake and their ability to escape macrophages. Conclusion: PTX-CPSO micelles could be a promising system for pulmonary targeting by intravenous administration.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

scholarly journals A biomimetic hybrid nanoplatform for encapsulation and precisely controlled delivery of theranostic agents

2015 ◽  
Vol 6 (1) ◽  
Author(s):  
Hai Wang ◽  
Pranay Agarwal ◽  
Shuting Zhao ◽  
Jianhua Yu ◽  
Xiongbin Lu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Encapsulation Efficiency ◽  
Near Infrared ◽  
Drug Loading ◽  
Eukaryotic Cell ◽  
Silica Matrix ◽  
High Drug ◽  
Theranostic Agents

Abstract Nanoparticles have demonstrated great potential for enhancing drug delivery. However, the low drug encapsulation efficiency at high drug-to-nanoparticle feeding ratios and minimal drug loading content in nanoparticle at any feeding ratios are major hurdles to their widespread applications. Here we report a robust eukaryotic cell-like hybrid nanoplatform (EukaCell) for encapsulation of theranostic agents (doxorubicin and indocyanine green). The EukaCell consists of a phospholipid membrane, a cytoskeleton-like mesoporous silica matrix and a nucleus-like fullerene core. At high drug-to-nanoparticle feeding ratios (for example, 1:0.5), the encapsulation efficiency and loading content can be improved by 58 and 21 times, respectively, compared with conventional silica nanoparticles. Moreover, release of the encapsulated drug can be precisely controlled via dosing near infrared laser irradiation. Ultimately, the ultra-high (up to ∼87%) loading content renders augmented anticancer capacity both in vitro and in vivo. Our EukaCell is valuable for drug delivery to fight against cancer and potentially other diseases.

In Silico Molecular Interaction Studies of Chitosan Polymer with Aromatase Inhibitor: Leads to Letrozole Nanoparticles for the Treatment of Breast Cancer

2020 ◽  
Vol 20 ◽  
Author(s):  
Keerti Mishra ◽  
Sant Kumar Verma ◽  
Pooja Ratre ◽  
Laxmi Banjare ◽  
Abhishek Jain ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Drug Delivery ◽  
Binding Energy ◽  
Molecular Interaction ◽  
In Silico ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Prolonged Release

Background: It takes lot more studies to evaluate the molecular interaction of nanoparticles with the drug, their drug delivery potential and release kinetics. Thus, we have taken in silico and in vitro approaches into the account for the evaluation of drug delivery ability of the chitosan nanoparticles. Objective: The present work was aimed to develop the interaction of chitosan nanoparticles with appropriate aromatase inhibitors using in-silico tools. Further, synthesis and characterization of chitosan nanoparticles having optimal binding energy and affinity between drug and polymer in terms of size, encapsulation efficiency was carried out. Methods: In current study, molecular docking was used to map the molecular interactions and estimation of binding energy involved between the nanoparticles and the drug molecules in silico. Letrozole is used as a model cytotoxic agent currently being used clinically, hence Letrozole loaded chitosan nanoparticles were formulated and characterized using photomicroscope, particle size analyzer, scanning electron microscope and fourier transform infra-red spectroscopy. Results: Letrozole had the second highest binding affinity within the core of chitosan with MolDock (-102.470) and Rerank (-81.084) scores. Further, it was investigated that formulated nanoparticles were having superior drug loading capacity and high encapsulation efficiency. In vitro drug release study exhibited prolonged release of the drug from chitosan nanoparticles. Conclusion: Results obtained from the in silico and in vitro studies suggest that Letrozole loaded nanoparticles are ideal for breast cancer treatment.

scholarly journals CARMUSTINE LOADED LACTOFERRIN NANOPARTICLES DEMONSTRATES AN ENHANCED ANTIPROLIFERATIVE ACTIVITY AGAINST GLIOBLASTOMA IN VITRO

2018 ◽  
Vol 10 (6) ◽  
pp. 234 ◽  
Author(s):  
Harikiran Athmakur ◽  
Anand Kumar Kondapi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Cellular Uptake ◽  
Stable Distribution ◽  
Drug Loading ◽  
Glioblastoma Cells ◽  
Treatment Regimens ◽  
Microscopic Studies

Objective: Despite sophisticated treatment regimens, there is no significant improvement in the mortality rates of glioblastoma due to insufficient dosage delivery, reoccurrence of tumors, higher systemic toxicity, etc. Since brain endothelial cells and glioblastoma cells express lactoferrin receptors, a target-specific drug delivery vehicle was developed using lactoferrin itself as a matrix, into which carmustine was loaded. The objective was to use carmustine loaded lactoferrin nanoparticles (CLN) to achieve higher therapeutic efficacy and target specificity compared to free carmustine.Methods: CLN were prepared using the Sol-oil method. The nanoparticles prepared were characterized for their size, shape, polydispersity, and stability using FESEM and DLS methods. Drug loading and drug releasing efficiencies were also estimated. Further, cellular uptake of nanoparticles and their antiproliferative efficacy against glioblastoma cells were evaluated.Results: Characterization of CLN showed that they were spherical with ≤ 41 nm diameter and exhibited homogeneously dispersed stable distribution. Loading efficiency of carmustine in CLN was estimated to be 43±3.7 %. Drug release from the nanoparticles was pH dependent with the maximum observed at pH 5. At physiological and gastric pH, drug release was lower, whereas maximum release was observed at endocytotic vesicular and around tumor extracellular pH. Confocal microscopic studies showed an active cellular uptake of nanoparticles. Results of antiproliferative analysis substantiated a higher antiproliferative effect for CLN compared to free carmustine.Conclusion: The results of the study demonstrated that CLN serves as a vital tool, in designing an effective treatment strategy for targeted drug delivery to glioblastoma.

scholarly journals Optimization Performance and Physical Stability of Ciprofloxacin HCL-Ca Alginate Microspheres: Effect of Different Concentration of Alginate and CaCl2

2020 ◽  
Vol 10 (01) ◽  
pp. 89-94
Author(s):  
Hariyadi DM ◽  
Hendradi E
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Physical Stability ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Local Drug Delivery ◽  
Control Drug ◽  
Lung Delivery ◽  
High Entrapment Efficiency

Inhalation treatment using antibiotics is an alternative for lung delivery. However, the therapeutic efficacy of inhaled drugs is limited by their rapid clearance in the lungs. Sustained release systems in the lungs can improve therapeutic outcomes of drugs because they can retain the drug load within the lungs and progressively release the drug locally at therapeutic levels. This study presents the formulation strategies to control drug release in the lungs using an alginate polymer-based microspheres system. The microsphere’s composition can be adjusted to modulate release and can encapsulate compounds with high loading. The pulmonary route is commonly used and has been well accepted as a portal for non-invasive drug delivery for many lung diseases. It is explored for decades as an alternative for systemic as well as local drug delivery. The present study explored the in vitro benefits of ciprofloxacin encapsulated in alginate microspheres. The studies included size, morphology, yield, drug loading, and encapsulation efficiency as well as stability. Current results showed small, smooth, and spherical ciprofloxacin-alginate microspheres were produced using aerosolization techniques. Small particles of less than 5μm were formed, which suitable for inhalation particles for lung delivery. High entrapment efficiency up to 95%, loadings of 80%, and a yield of 89% were also showed from microspheres. It was confirmed that all microspheres were stably indicated by no significant changes in morphology, organoleptic, and drug content after 30 days of storage. The recent promising characteristics of microspheres for pulmonary delivery will need further evaluation of the potency against microorganisms in lung disease.

Minocycline hydrochloride loaded mPEG-PCLA membranes: Preparation and in vitro evaluation for periodontitis therapy

2021 ◽  
pp. 088391152199279
Author(s):  
Ningtao Wang ◽  
Zhengmei Huang ◽  
Shenchun Wang ◽  
Meidong Lang ◽  
Xiuyin Zhang
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Membrane Surface ◽  
Local Treatment ◽  
In Vitro Release ◽  
Periodontal Pathogen ◽  
Antibacterial Drug ◽  
Periodontal Ligament Fibroblasts ◽  
Minocycline Hydrochloride

This study was aimed at alleviating shortcomings in the treatment of periodontitis by preparation of a biopolymer membrane loaded with minocycline hydrochloride (MH) inserted into periodontal pockets to treat infections. Monomethoxy-poly (ethylene glycol)-poly (ε-caprolactone-co-L-lactide) (mPEG-PCLA) is a biocompatible and biodegradable amphiphilic block copolymer. It, therefore, has attracted considerable attention in drug delivery systems and periodontal treatment. We chose it as a membrane material for MH-drug loading. The MH-loaded membranes were prepared by the solvent casting technique with the content of 5, 8 and 10 wt.%, respectively. Fourier transform infrared spectra (FTIR) revealed no interaction between MH and polymer. The drug-loaded membrane surface morphology was investigated by scanning electron microscopy (SEM). In vitro release studies showed that the initial drug release exceeded 40% within 24 h, followed by a sustained release for up to 2 weeks, which would enable the therapeutic level to maintain over a longer time. The antibacterial activity studies in vitro demonstrated a positive effect on the periodontal pathogen. MH drug-loaded membranes have no adverse effect on the growth of periodontal ligament fibroblasts in the MTT test. The study suggests that mPEG-PCLA membranes containing MH are a potential antibacterial drug delivery system for local treatment of periodontitis.

Study on the Antibacterial Performance of the Antibacterial Shutter Blades

2013 ◽  
Vol 815 ◽  
pp. 333-338
Author(s):  
Ming Li Liu ◽  
Chun Feng Li ◽  
Yun Long Wang ◽  
Kai Lu ◽  
Jiu Yin Pang ◽  
...  
Keyword(s):  
Antibacterial Agent ◽  
Antibacterial Agents ◽  
Drug Loading ◽  
Antibacterial Properties ◽  
Water Soluble ◽  
Single Factor ◽  
Antibacterial Performance ◽  
Loading Amount ◽  
Single Factor Experiment ◽  
Impregnation Solution

This study used Ag-embedded nanoTiO2, xylan and water-soluble Chitosan as antibacterial agents, respectively prepared shutter blades through the treating solution of the different concentration and the different drug loading amount of the poplar veneer. Through a single factor experiment, this paper analyzes that the different antibacterial agent, concentration of antibacterial agent and the drug loading amount have an effect on the antibacterial properties of the shutter blades. The results show that the order of antibacterial performance of the shutter blades impregnated antibacterial agents is the Ag-embedded nanoTiO2, Chitosan, Xylan. Comprehensiv-ely thought the antibacterial properties and economic index, the optimal concentration of the Ag-embedded nanoTiO2 impregnation solution is 1%.

scholarly journals Chitosan/poly(lactic-co-glycolic)acid Nanoparticle Formulations with Finely-Tuned Size Distributions for Enhanced Mucoadhesion

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 95
Author(s):  
Feipeng Yang ◽  
Maleen Cabe ◽  
Hope A. Nowak ◽  
Kelly A. Langert
Keyword(s):  
Drug Delivery ◽  
Aqueous Phase ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Delivery Systems ◽  
Intranasal Delivery ◽  
Brain Drug Delivery ◽  
Size Groups ◽  
Formulation Parameters

Non-parenteral drug delivery systems using biomaterials have advantages over traditional parenteral strategies. For ocular and intranasal delivery, nanoparticulate systems must bind to and permeate through mucosal epithelium and other biological barriers. The incorporation of mucoadhesive and permeation-enhancing biomaterials such as chitosan facilitate this, but tend to increase the size and polydispersity of the nanoparticles, making practical optimization and implementation of mucoadhesive nanoparticle formulations a challenge. In this study, we adjusted key poly(lactic-co-glycolic) acid (PLGA) nanoparticle formulation parameters including the organic solvent and co-solvent, the concentration of polymer in the organic phase, the composition of the aqueous phase, the sonication amplitude, and the inclusion of chitosan in the aqueous phase. By doing so, we prepared four statistically unique size groups of PLGA NPs and equally-sized chitosan-PLGA NP counterparts. We loaded simvastatin, a candidate for novel ocular and intranasal delivery systems, into the nanoparticles to investigate the effects of size and surface modification on drug loading and release, and we quantified size- and surface-dependent changes in mucoadhesion in vitro. These methods and findings will contribute to the advancement of mucoadhesive nanoformulations for ocular and nose-to-brain drug delivery.

scholarly journals Development and characterization of phytosterol nanoemulsions and self-microemulsifying drug delivery systems

2019 ◽  
Author(s):  
Yuan Chuanxun ◽  
Zhang Xueru ◽  
Jin Risheng
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Drug Loading ◽  
In Vitro Release ◽  
Pharmacokinetic Analysis ◽  
Polyethylene Glycol 400 ◽  
Hydrogenated Castor Oil ◽  
Release Curve ◽  
Tween 60

AbstractThe aim of this study is to develop a self microemulsion drug delivery system for phytosterols to improve the solubility and bioavailability. The results showed that the formulation of phytosterol self-microemulsion is: lemon essential oil in oil phase, polyoxyethylene hydrogenated castor oil 40 and Tween 60 in emulsifier, polyethylene glycol 400 in co-emulsifier, Km = 7:3, Kp = 3:1, Ke = 50%. The drug loading of phytosterol self-microemulsion prepared by this method was 87.22 mg/g, encapsulation efficiency was 89.65%, particle size was 48.85nm, potential was −12.863mV. In vitro release experiment showed that the release of phytosterols in microemulsion was more than 90%, and the release curve was in accordance with the first-order kinetics equation. The pharmacokinetic analysis of PSSM synthesized by this method shows that PSSM can increase the bioavailability of PS more than three times, so it is necessary to do more in-depth research on the self-microemulsion delivery system of phytosterols.

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