Four-fold Channel-Nicked Human Ferritin Nanocages for Active Drug Loading and pH-Responsive Drug Release

The development of controlled drug delivery systems based on bio-renewable materials is an emerging strategy. In this work, a controlled drug delivery system based on mesoporous oxidized cellulose beads (OCBs) was successfully developed by a facile and green method. The introduction of the carboxyl groups mediated by the TEMPO(2,2,6,6-tetramethylpiperidine-1-oxyradical)/NaClO/NaClO2 system presents the pH-responsive ability to cellulose beads, which can retain the drug in beads at pH = 1.2 and release at pH = 7.0. The release rate can be controlled by simply adjusting the degree of oxidation to achieve drug release at different locations and periods. A higher degree of oxidation corresponds to a faster release rate, which is attributed to a higher degree of re-swelling and higher hydrophilicity of OCBs. The zero-order release kinetics of the model drugs from the OCBs suggested a constant drug release rate, which is conducive to maintaining blood drug concentration, reducing side effects and administration frequency. At the same time, the effects of different model drugs and different drug-loading solvents on the release behavior and the physical state of the drugs loaded in the beads were studied. In summary, the pH-responsive oxidized cellulose beads with good biocompatibility, low cost, and adjustable release rate have shown great potential in the field of controlled drug release.

Download Full-text

Schiff-Linked PEGylated Doxorubicin Prodrug Forming pH-Responsive Nanoparticles With High Drug Loading and Effective Anticancer Therapy

Frontiers in Oncology ◽

10.3389/fonc.2021.656717 ◽

2021 ◽

Vol 11 ◽

Author(s):

Jian Song ◽

Bingbing Xu ◽

Hui Yao ◽

Xiaofang Lu ◽

Yang Tan ◽

...

Keyword(s):

Drug Release ◽

Tumor Cells ◽

Drug Loading ◽

Drug Carriers ◽

Anticancer Therapy ◽

Therapeutic Effects ◽

Ph Responsive ◽

High Drug ◽

High Drug Loading ◽

Mcf 7

Developing efficacious drug delivery systems for targeted cancer chemotherapy remains a major challenge. Here we demonstrated a kind of pH-responsive PEGylated doxorubicin (DOX) prodrug via the effective esterification and Schiff base reactions, which could self-assemble into the biodegradable micelles in aqueous solutions. Owing to low pH values inside the tumor cells, these PEG-Schiff-DOX nanoparticles exhibited high drug loading ability and pH-responsive drug release behavior within the tumor cells or tissues upon changes in physical and chemical environments, but they displayed good stability at physiological conditions for a long period. CCK-8 assay showed that these PEGylated DOX prodrugs had a similar cytotoxicity to the MCF-7 tumor cells as the free DOX drug. Moreover, this kind of nanoparticle could also encapsulate small DOX drugs with high drug loading, sufficient drug release and enhanced therapeutic effects toward MCF-7 cells, which will be benefited for developing more drug carriers with desirable functions for clinical anticancer therapy.

Download Full-text

Integrin-targeted pH-responsive micelles for enhanced efficiency of anticancer treatment in vitro and in vivo

Nanoscale ◽

10.1039/c4nr07435a ◽

2015 ◽

Vol 7 (10) ◽

pp. 4451-4460 ◽

Cited By ~ 20

Author(s):

Jinjian Liu ◽

Hongzhang Deng ◽

Qiang Liu ◽

Liping Chu ◽

Yumin Zhang ◽

...

Keyword(s):

Drug Release ◽

Tumor Targeting ◽

Drug Loading ◽

Ph Responsive ◽

Tumor Treatment ◽

Anticancer Treatment ◽

Drug Loading Efficiency ◽

Targeting Ability

Integrin-targeted pH-responsive micelles were synthesized with an enhanced drug-loading efficiency, tumor-targeting ability and pH-controlled intracellular drug release for enhanced tumor treatment.

Download Full-text

Determination of Drug Loading Efficiency and Drug Release of Loperamide from Polymeric Nanocarriers

10.26226/morressier.57d6b2b6d462b8028d88dafe ◽

2016 ◽

Author(s):

Javier Morales

Keyword(s):

Drug Release ◽

Drug Loading ◽

Polymeric Nanocarriers ◽

Loading Efficiency ◽

Drug Loading Efficiency

Download Full-text

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.5 ◽

2020 ◽

Vol 12 (2) ◽

pp. 4474-4491

Author(s):

Rajkumar Aland ◽

Ganesan M ◽

P. Rajeswara Rao ◽

Bhikshapathi D. V. R. N.

Keyword(s):

Particle Size ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Tem Analysis ◽

In Vitro Drug Release ◽

Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements. In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Download Full-text

Nanostructures for pH-sensitive Drug Delivery and Magnetic Resonance Contrast Enhancement Systems

Current Medicinal Chemistry ◽

10.2174/0929867324666170406110642 ◽

2018 ◽

Vol 25 (25) ◽

pp. 3036-3057 ◽

Cited By ~ 6

Author(s):

Xiao Sun ◽

Guilong Zhang ◽

Zhengyan Wu

Keyword(s):

Drug Delivery ◽

Magnetic Resonance ◽

Drug Release ◽

Contrast Enhancement ◽

General Strategy ◽

Ph Responsive ◽

Physicochemical Changes ◽

Magnetic Resonance Contrast ◽

Resonance Contrast ◽

Magnetic Resonance Contrast Enhancement

According to the differences of microenvironments between tumors and healthy tissues, if the anticancer drugs or magnetic resonance contrast agents (MRCAs) can be controlled to precisely match physiological needs at targeted tumor sites, it is expected to acquire better therapeutic efficacy and more accurate diagnosis. Over the decade, stimuli-responsive nanomaterials have been a research hotspot for cancer treatment and diagnosis because they show many excellent functions, such as in vivo imaging, combined targeting drug delivery and systemic controlled release, extended circulation time, etc. Among the various stimuli nanosystems, pH-stimuli mode is regarded as the most general strategy because of solid tumors acidosis. When exposed to weakly acidic tumor microenvironment, pH-responsive nanoplatforms can generate physicochemical changes for their structure and surface characteristics, causing drug release or contrast enhancement. In this review, we focused on the designs of various pH-responsive nanoplatforms and discussed the mechanisms of controlled drug release or switch on-off in MRCAs. This review also discussed the efficacy of cellular internalization for these nanoplatforms via endocytosis of acidic tumor cell. Meanwhile, nanoplatforms response to acidic intracellular pH (such as endosome, lysosome) are discussed, along with approaches for improving drug release performance and magnetic resonance contrast enhancement. A greater understanding of these pH-responsive nanoplatforms will help design more efficient nanomedicine to address the challenges encountered in conventional diagnosis and chemotherapy.

Download Full-text

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

Current Medicinal Chemistry ◽

10.2174/0929867326666190624155938 ◽

2020 ◽

Vol 27 (22) ◽

pp. 3623-3656 ◽

Cited By ~ 1

Author(s):

Bruno Fonseca-Santos ◽

Patrícia Bento Silva ◽

Roberta Balansin Rigon ◽

Mariana Rillo Sato ◽

Marlus Chorilli

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Drug Loading ◽

Average Particle Size ◽

Delivery Systems ◽

Average Particle ◽

Minor Importance ◽

Routes Of Administration ◽

Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

Download Full-text