scholarly journals Synthesis and Characterization of Stearic Acid-Beclomethasone Dipropionate Conjugates with the Potential for Improving Loading Capacity in Lipid-based Nanoparticles

Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu

<p>Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.</p>

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu

<p>Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.</p>


RSC Advances ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 7163-7169
Author(s):  
Xin Li ◽  
Danlin Zeng ◽  
Ping Ke ◽  
Guanghui Wang ◽  
Dengke Zhang

A novel magnetic microsphere was prepared by the simple microemulsion polymerization for protein drug delivery systems. This magnetic microsphere exhibited good magnetism and superior drug loading capacity and evident sustained-release performance.


2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Jinglei Du ◽  
Qiang Li ◽  
Lin Chen ◽  
Shicai Wang ◽  
Li Zhang ◽  
...  

A dual-targeting drug delivery system (DTDDS) with magnetic targeting and active targeting was obtained to improve the targeting and drug-loading capacity of magnetic drug nanocarriers. An ultraviolet-visible spectrophotometer and flow cytometry were used to investigate the drug-loading and release capacity, cytotoxicity, and inhibition of tumor cell proliferation, separately. Results show that DTDDS has obvious magnetic characteristics, on which the modification amount of folic acid is 64.82 mg g-1. Doxorubicin was taken as a template drug to evaluate its drug-loading capacity, which was as high as 577.12 mg g-1. Good biocompatibility and low cytotoxicity of DTDDS were further confirmed. Moreover, DTDDS can target the folate receptor on the surface of HeLa cells and deliver doxorubicin into HeLa cells, thereby increasing the proliferation inhibition for cancer cells. Therefore, this new dual-targeting drug delivery system shows potential in significantly reducing the toxic side effects of chemotherapy and improving chemotherapy efficiency.


Polymers ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 1621
Author(s):  
Beini Zeng ◽  
Xungai Wang ◽  
Nolene Byrne

Cellulose beads were successfully prepared from waste denim using a dissolution-regeneration approach with ionic liquids as the dissolving solvent. Cellulose beads with different morphologies were achieved by altering the dissolving and coagulating solvents. The morphological differences were quantified by N2 physisorption. The impact of morphology on the cellulose beads’ potential application was investigated in the context of drug loading and release. The results show that the fibrous morphology showed a better loading capacity than the globular analogue due to its higher surface area and pore volume.


RSC Advances ◽  
2019 ◽  
Vol 9 (61) ◽  
pp. 35566-35578 ◽  
Author(s):  
Subhankar Mukhopadhyay ◽  
Hanitrarimalala Veroniaina ◽  
Tadious Chimombe ◽  
Lidong Han ◽  
Wu Zhenghong ◽  
...  

Protean mesoporous silica nanoparticles are propitious candidates over decades for nanoscale drug delivery systems due to their unique characteristics, including changeable pore size, mesoporosity, high drug loading capacity and biodegradability.


Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3455
Author(s):  
Elisabetta Rosa ◽  
Carlo Diaferia ◽  
Enrico Gallo ◽  
Giancarlo Morelli ◽  
Antonella Accardo

Recently, nanogels have been identified as innovative formulations for enlarging the application of hydrogels (HGs) in the area of drug delivery or in diagnostic imaging. Nanogels are HGs-based aggregates with sizes in the range of nanometers and formulated in order to obtain injectable preparations. Regardless of the advantages offered by peptides in a hydrogel preparation, until now, only a few examples of peptide-based nanogels (PBNs) have been developed. Here, we describe the preparation of stable PBNs based on Fmoc-Phe-Phe-OH using three different methods, namely water/oil emulsion (W/O), top-down, and nanogelling in water. The effect of the hydrophilic–lipophilic balance (HLB) in the formulation was also evaluated in terms of size and stability. The resulting nanogels were found to encapsulate the anticancer drug doxorubicin, chosen as the model drug, with a drug loading comparable with those of the liposomes.


Polymers ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 2200
Author(s):  
Yuanyuan Wang ◽  
Yongyue Li ◽  
Jinghua Gong ◽  
Jinghong Ma

Here, we report a novel thermo-triggered-releasing microcapsule for liposoluble drug delivery. Monodisperse microcapsules with a poly(N-isopropylacrylamide-co-methacrylic acid) hydrogel shell and an oil core were successfully fabricated by a double coaxial microfluidic device. Fluorescent dye Lumogen Red F300 as a model liposoluble drug was dissolved in the oil core with controllable loading capacity. The volume phase transition temperature (VPTT) of the microcapsule was adjusted by copolymerizing with the hydrophilic methacrylic acid. The in vitro release study demonstrates that the shells shrink, leading to the thermo-triggered release of the model drug from the microcapsules at the environmental temperature above the VPTT, while the swollen hydrogel shells can protect the encapsulated drug from leakage and contamination below the VPTT. The proposed microcapsule is a promising liposoluble drug delivery system with controllable loading and smart thermo-triggered release.


Nanomedicine ◽  
2020 ◽  
Vol 15 (5) ◽  
pp. 489-509
Author(s):  
Dong Shen ◽  
Yan Shen ◽  
Qian Chen ◽  
Bin Huang ◽  
Yedong Mi ◽  
...  

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.


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