scholarly journals Stable Formulations of Peptide-Based Nanogels

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3455
Author(s):  
Elisabetta Rosa ◽  
Carlo Diaferia ◽  
Enrico Gallo ◽  
Giancarlo Morelli ◽  
Antonella Accardo
Keyword(s):  
Drug Delivery ◽  
Diagnostic Imaging ◽  
Anticancer Drug ◽  
Drug Loading ◽  
Top Down ◽  
Oil Emulsion ◽  
Hydrophilic Lipophilic Balance ◽  
Model Drug

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.

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

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Pulmonary Delivery ◽  
Dynamics Simulation ◽  
Loading Capacity ◽  
Technology Platform ◽  
New Type ◽  
Model Drug

<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>

scholarly journals Anticancer drug nanomicelles formed by self-assembling amphiphilic dendrimer to combat cancer drug resistance

2015 ◽  
Vol 112 (10) ◽  
pp. 2978-2983 ◽  
Author(s):  
Tuo Wei ◽  
Chao Chen ◽  
Juan Liu ◽  
Cheng Liu ◽  
Paola Posocco ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Resistance ◽  
Cancer Therapy ◽  
Drug Delivery System ◽  
Anticancer Drug ◽  
Delivery System ◽  
Drug Carrier ◽  
Drug Loading ◽  
Cancer Drug ◽  
Self Assembling

Drug resistance and toxicity constitute challenging hurdles for cancer therapy. The application of nanotechnology for anticancer drug delivery is expected to address these issues and bring new hope for cancer treatment. In this context, we established an original nanomicellar drug delivery system based on an amphiphilic dendrimer (AmDM), which could generate supramolecular micelles to effectively encapsulate the anticancer drug doxorubicin (DOX) with high drug-loading capacity (>40%), thanks to the unique dendritic structure creating large void space for drug accommodation. The resulting AmDM/DOX nanomicelles were able to enhance drug potency and combat doxorubicin resistance in breast cancer models by significantly enhancing cellular uptake while considerably decreasing efflux of the drug. In addition, the AmDM/DOX nanoparticles abolished significantly the toxicity related to the free drug. Collectively, our studies demonstrate that the drug delivery system based on nanomicelles formed with the self-assembling amphiphilic dendrimer constitutes a promising and effective drug carrier in cancer therapy.

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

2021 ◽  
Author(s):  
Shishuai Dang ◽  
Zhengwei Huang ◽  
Ying Huang ◽  
Xin Pan ◽  
Chuanbin Wu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Beclomethasone Dipropionate ◽  
Drug Loading ◽  
Pulmonary Delivery ◽  
Dynamics Simulation ◽  
Loading Capacity ◽  
Technology Platform ◽  
New Type ◽  
Model Drug

<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>

Poly(N-isopropylacrylamide)-b-Poly(L-lysine)-b-Poly(L-histidine) Triblock Amphiphilic Copolymer Nanomicelles for Dual-Responsive Anticancer Drug Delivery

2020 ◽  
Vol 20 (11) ◽  
pp. 6959-6967
Author(s):  
Rimesh Augustine ◽  
Dae-Kyoung Kim ◽  
Ho An Kim ◽  
Jae Ho Kim ◽  
Il Kim
Keyword(s):  
Drug Delivery ◽  
Anticancer Drug ◽  
Drug Loading ◽  
Anticancer Drug Delivery ◽  
Dual Responsive ◽  
Micellar Aggregates ◽  
Reversible Addition ◽  
Hydrogen Carbonate ◽  
Copolymer Micelle

A series of ABC triblock poly(N-isopropylacrylamide)75-block-poly(L-lysine)35-block-poly(L-histidine)n (p(NIPAM)75-b-p(Lys)35-b-p(His)N) (N = 35,50,75,100) copolymer bio-conjugates were prepared by combining reversible addition-fragmentation chain transfer polymerization and fast ring-opening polymerization of N-carboxyanhydride a-amino acid using 1,3-dicyclohexylimidazolium hydrogen carbonate as a catalyst. All the resulting triblock copolymers self-assembled into spherical micellar aggregates in aqueous solution, irrespective of the chain length of the histidine block. The micellar aggregates encapsulated the anticancer drug doxorubicin (Dox) and exhibited high drug loading efficiency. Temperature and pH stimuli were applied to investigate the controlled release of Dox. The non-cytotoxic nature of the polymers was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cellular uptake of the Dox-loaded micelles revealed that the micelles successfully release Dox in cancer cells in response to pH- and temperature-induced morphological change. In-vitro studies further confirmed that the Dox-loaded triblock copolymer micelle is an excellent platform for drug delivery.

Evaluation of Potential of Uncoated Mesoporous Silica Particles for Drug Delivery Applications

2021 ◽  
Vol 875 ◽  
pp. 366-372
Author(s):  
Tayyab Ali Khan ◽  
Syed Mujtaba Ul Hassan ◽  
Hassan Waqas ◽  
Jamil Ahmad ◽  
Ahmat Khurshid ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Drug Loading ◽  
Sol Gel ◽  
Cancer Cell Line ◽  
Silica Particles ◽  
Atomic Force ◽  
Drug Delivery Applications ◽  
Model Drug ◽  
Average Size

The drug loading capability and inherent cytotoxicity of mesoporous silica particles are two prime considerations for targeted drug delivery applications. In current study, uncoated mesoporous silica (UMS) carrier particles were synthesized by sol-gel emulsion approach. The morphology and structure of UMS was thoroughly characterized using atomic force microscope (AFM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and Brunauer–Emmett–Teller (BET). The scanning electron microscopy (SEM) and dynamic light scattering (DLS) measurements reveal that mono dispersed silica particles have an average size of 250 nm with narrow size distribution. The pore size was measured as 47nm. Concentration dependent biocompatibility of UMS was evaluated using MTT assay with Hep-2c cancer cell line and cell viability of ~65% at concentrations of 7.5 nM was observed. Finally, the drug loading capability of UMS carrier was studied using ibuprofen as a model drug.

scholarly journals Synthesis and Characterization of Starch-Graft-Acrylamide Hydrogel for Oral Drug Delivery

2020 ◽  
Vol 27 (2) ◽  
pp. 16-21
Author(s):  
H. Musa ◽  
Y. Musa ◽  
M. Suleiman
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Oral Drug ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Swelling Capacity ◽  
Model Drug ◽  
Polymerization Method

In this research, starch was extracted from fresh sweet potato and was used to prepare starch-g-acrylamide hydrogel using free radical polymerization method with potassium per sulphate and N’N-Methylene bisacrylamide as initiator and cross-linker, respectively. The swelling capacity and pH sensitivity of the synthesized hydrogel were investigated in solutions of various pH (1-12). The drug loading and release experiment was also carried out using promethazine (PMZ) as the model drug at 25oC and 37oC, respectively while the release study was carried out in an enzyme-free simulated gastric intestinal fluid (SGF) and simulated intestinal fluid (SIF). The result showed a 905% swelling at pH 11, suggesting increased swelling capacity at higher pH values. Drug loading result indicated 99% of the drug was entrapped by the hydrogel as confirmed by UV-visible spectrophotometry. SIF and SGF Simulation indicated a 24% and 9% drug release for the first ten hours. At the end of 48 hours the release was 96% and 89%, respectively indicating the hydrogel released more promethazine in SIF than in SGF. The results obtained in this work suggest that starch-graft-acrylamide hydrogel is a potential vehicle for oral drug delivery. Keywords: Starch, Acrylamide, Hydrogel, Drug delivery.

scholarly journals Conjugation of a smart polymer to doxorubicin through a pH-responsive bond for targeted drug delivery and improving drug loading on graphene oxide

RSC Advances ◽  
2021 ◽  
Vol 11 (31) ◽  
pp. 18809-18817
Author(s):  
Ali Bina ◽  
Heidar Raissi ◽  
Hassan Hashemzadeh ◽  
Farzaneh Farzad
Keyword(s):  
Drug Delivery ◽  
Graphene Oxide ◽  
Anticancer Drug ◽  
Targeted Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Ph Responsive ◽  
Smart Polymer ◽  
Anticancer Drug Delivery ◽  
Targeted Drug

Polymeric nanoparticles have emerged as efficient carriers for anticancer drug delivery because they can improve the solubility of hydrophobic drugs and also can increase the bio-distribution of drugs throughout the bloodstream.

scholarly journals Artificial exosomes for translational nanomedicine

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Yong-Jiang Li ◽  
Jun-Yong Wu ◽  
Jihua Liu ◽  
Wenjie Xu ◽  
Xiaohan Qiu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Quality Control ◽  
Lipid Bilayer ◽  
Drug Loading ◽  
Membrane Vesicles ◽  
Bilayer Membrane ◽  
Lipid Bilayer Membrane ◽  
Future Perspectives ◽  
Top Down ◽  
Production Standard

AbstractExosomes are lipid bilayer membrane vesicles and are emerging as competent nanocarriers for drug delivery. The clinical translation of exosomes faces many challenges such as massive production, standard isolation, drug loading, stability and quality control. In recent years, artificial exosomes are emerging based on nanobiotechnology to overcome the limitations of natural exosomes. Major types of artificial exosomes include ‘nanovesicles (NVs)’, ‘exosome-mimetic (EM)’ and ‘hybrid exosomes (HEs)’, which are obtained by top-down, bottom-up and biohybrid strategies, respectively. Artificial exosomes are powerful alternatives to natural exosomes for drug delivery. Here, we outline recent advances in artificial exosomes through nanobiotechnology and discuss their strengths, limitations and future perspectives. The development of artificial exosomes holds great values for translational nanomedicine.

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