Targeted delivery, drug release strategies, and toxicity study of polymeric drug nanocarriers

2020 ◽  
Author(s):  
Payam Abasian ◽  
Sepideh Shakibi ◽  
Mohammad Saeed Maniati ◽  
Saied Nouri Khorasani ◽  
Shahla Khalili
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Toxicity Study ◽  
Polymeric Drug ◽  
Drug Nanocarriers

pH Dependent Release Potential of Natural Polymers in Sustained Release of Ornidazole From Colon Targeted Delivery System)

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Sharma Pankaj ◽  
Tailang Mukul
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Guar Gum ◽  
Acidic Environment ◽  
Natural Polymers ◽  
Weight Variation ◽  
Curve Determination ◽  
Preformulation Studies

The aim of present work was to prepare colon specific delivery system of Ornidazole using different ratio of shellac, zein and guar gum. From study of various literature it revealed that shellac, zein and guar gum released drug from dosage form at the pH of 6.9, 11.5, 7-9 respectively. The main problem associated with colon targeted drug delivery system is degradation of drug in the acidic environment of stomach to circumvent the present problem different combinations of shellac, zein and guar gum were employed in the formulation of colon targeted tablet. Several preformulation parameters were determined such as melting point, FTIR spectroscopy, preparation of calibration curve, determination of λmax and partition coefficient. After the preformulation studies, next steps were preparation of core tablets, evaluation of core of tablets and coating of tablets. The data obtained from preformulation study seven formulations were developed and evaluated for various parameters. Based on evaluated parameter such as weight variation, friability, dissolution study, invitro drug release etc. the F7 formulation show better results colon targeted tablets. Drug content in F7 formulation was 95% and drug release after 6 hrs was 96%. Formulation containing combination of shellac, zein and guar gum released least amount of drug in the acidic environment of stomach and released most of the drug in colon. It is evide

The Smart Dual-Stimuli Responsive Nanoparticles for Controlled AntiTumor Drug Release and Cancer Therapy

2020 ◽  
Vol 20 ◽  
Author(s):  
Feng Wu ◽  
Fei Qiu ◽  
Siew Anthony Wai-Keong ◽  
Yong Diao
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Drug Release ◽  
Targeted Delivery ◽  
Relevant Information ◽  
Therapeutic Effects ◽  
Stimuli Responsive ◽  
Control Effect ◽  
Chemotherapy Drugs ◽  
Excellent Control

Background: In recent years, the emergence of stimuli-responsive nanoparticles makes drug delivery more efficient. As an intelligent and effective targeted delivery platform, it can reduce the side effects generated during drug transportation while enhancing the treatment efficacy. The stimuli-responsive nanoparticles can respond to different stimuli at corresponding times and locations to deliver and release their drugs and associated therapeutic effects. Objective: This review aims to inform researchers on the latest advances in the application of dual-stimuli responsive nanoparticles in precise drug delivery, with special attention to their design, drug release properties, and therapeutic effects. Syntheses of nanoparticles with simultaneous or sequential responses to two or more stimuli (pH-redox, pH-light, redoxlight, temperature-magnetic, pH-redox-temperature, redox-enzyme-light, etc.) and the applications of such responsivity properties for drugs control and release have become a hot topic of recent research. Methods: A database of relevant information for the production of this review was sourced, screened and analyzed from Pubmed, Web of Science, SciFinder by searching for the following keywords: “dual-stimuli responsive”, “controlled release”, “cancer therapy”, “synergistic treatment”. Results: Notably, the nanoparticles with dual-stimuli responsive function have an excellent control effect on drug delivery and release, playing a crucial part in the treatment of tumors. They can improve the encapsulation and delivery efficiency of hydrophobic chemotherapy drugs, combine chemo-photothermal therapies, apply imaging function in the diagnosis of tumors and even conduct multi-drugs delivery to overcome multi-drugs resistance (MDR). Conclusion: With the development of smart dual-stimuli responsive nanoparticles, cancer treatment methods will become more diverse and effective. All the stimuli-responsive nanoparticles functionalities exhibited their characteristics individually within the single nanosystem.

scholarly journals Cefotaxime Loaded Polycaprolactone Based Polymeric Nanoparticles with Antifouling Properties for In-Vitro Drug Release Applications

Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2180
Author(s):  
Sana Javaid ◽  
Nasir M. Ahmad ◽  
Azhar Mahmood ◽  
Habib Nasir ◽  
Mudassir Iqbal ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
In Vitro Release ◽  
Bacterial Strains ◽  
In Vitro Drug Release ◽  
Antifouling Activity ◽  
Polymeric Drug ◽  
Pure Drug ◽  
Average Size

The objective of the present study was to achieve the successful encapsulation of a therapeutic agent to achieve antifouling functionality regarding biomedical applications. Considering nanotechnology, drug-loaded polycaprolactone (PCL)-based nanoparticles were prepared using a nano-precipitation technique by optimizing various process parameters. The resultant nano-formulations were investigated for in vitro drug release and antifouling applications. The prepared particles were characterized in terms of surface morphology and surface properties. Optimized blank and drug-loaded nanoparticles had an average size of 200 nm and 216 nm, respectively, with associated charges of −16.8 mV and −11.2 mV. Studies of the in vitro release of drug were carried out, which showed sustained release at two different pH, 5.5 and 7.4 Antifouling activity was observed against two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. The zone of inhibition of the optimized polymeric drug-loaded nanoparticle F-25 against both strains were compared with the pure drug. The gradual pH-responsive release of antibiotics from the biodegradable polymeric nanoparticles could significantly increase the efficiency and pharmacokinetics of the drug as compared to the pure drug. The acquired data significantly noted that the resultant nano-encapsulation of antifouling functionality could be a promising candidate for topical drug delivery systems and skin applications.

scholarly journals Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kenneth Chibuzor Ofokansi ◽  
Franklin Chimaobi Kenechukwu
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Local Treatment ◽  
Wet Granulation ◽  
Formulation Development ◽  
Swelling Properties ◽  
Interpolyelectrolyte Complexes ◽  
Bowel Diseases

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

scholarly journals Injectable Thermo-Sensitive Chitosan Hydrogel Containing CPT-11-Loaded EGFR-Targeted Graphene Oxide and SLP2 shRNA for Localized Drug/Gene Delivery in Glioblastoma Therapy

2020 ◽  
Vol 21 (19) ◽  
pp. 7111 ◽  
Author(s):  
Yu-Jen Lu ◽  
Yu-Hsiang Lan ◽  
Chi-Cheng Chuang ◽  
Wan-Ting Lu ◽  
Li-Yang Chan ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Gene Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Drug Formulation ◽  
Treatment Modalities ◽  
Gene Delivery System ◽  
Optimal Drug

In this study, we aimed to develop a multifunctional drug/gene delivery system for the treatment of glioblastoma multiforme by combining the ligand-mediated active targeting and the pH-triggered drug release features of graphene oxide (GO). Toward this end, we load irinotecan (CPT-11) to cetuximab (CET)-conjugated GO (GO-CET/CPT11) for pH-responsive drug release after endocytosis by epidermal growth factor receptor (EGFR) over-expressed U87 human glioblastoma cells. The ultimate injectable drug/gene delivery system was designed by co-entrapping stomatin-like protein 2 (SLP2) short hairpin RNA (shRNA) and GO-CET/CPT11 in thermosensitive chitosan-g-poly(N-isopropylacrylamide) (CPN) polymer solution, which offers a hydrogel depot for localized, sustained delivery of the therapeutics after the in situ formation of CPN@GO-CET/CPT11@shRNA hydrogel. An optimal drug formulation was achieved by considering both the loading efficiency and loading content of CPT-11 on GO-CET. A sustained and controlled release behavior was found for CPT-11 and shRNA from CPN hydrogel. Confocal microscopy analysis confirmed the intracellular trafficking for the targeted delivery of CPT-11 through interactions of CET with EGFR on the U87 cell surface. The efficient transfection of U87 using SLP2 shRNA was achieved using CPN as a delivery milieu, possibly by the formation of shRNA/CPN polyplex after hydrogel degradation. In vitro cell culture experiments confirmed cell apoptosis induced by CPT-11 released from acid organelles in the cytoplasm by flow cytometry, as well as reduced SLP2 protein expression and inhibited cell migration due to gene silencing. Finally, in vivo therapeutic efficacy was demonstrated using the xenograft of U87 tumor-bearing nude mice through non-invasive intratumoral delivery of CPN@GO-CET/CPT11@shRNA by injection. Overall, we have demonstrated the novelty of this thermosensitive hydrogel to be an excellent depot for the co-delivery of anticancer drugs and siRNA. The in situ forming hydrogel will not only provide extended drug release but also combine the advantages offered by the chitosan-based copolymer structure for siRNA delivery to broaden treatment modalities in cancer therapy.

Colon-Targeted Therapy of Tacrolimus (FK506) in the Treatment of Experimentally Induced Colitis

Pharmacology ◽  
2020 ◽  
Vol 105 (9-10) ◽  
pp. 541-549 ◽  
Author(s):  
Ahmed S. Ali ◽  
Abid A. Altayari ◽  
Lateef M. Khan ◽  
Sameer E. Alharthi ◽  
Osama A. Ahmed ◽  
...  
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Intestinal Inflammation ◽  
Rescue Therapy ◽  
Immunosuppressive Agent ◽  
Water Emulsion ◽  
Distribution Study ◽  
In Vivo Distribution ◽  
Oil In Water Emulsion

<b><i>Background/Aims:</i></b> Inflammatory bowel disease is a chronic or remitting/relapsing intestinal inflammation, which comprises Crohn’s disease and ulcerative colitis (UC). Severe UC is a life-threatening condition that requires corticosteroids (CS) as a first-line rescue therapy. Some patients are refractory to CS and may require alternative immunosuppressive therapy. Oral tacrolimus (FK506), an immunosuppressive agent, has been reported to be effective in the management of severe refractory UC, but it can cause serious adverse effects. This work aims to study the effect of tacrolimus delivered by a colon-targeted delivery system (CTDS) in a dextran sulfate sodium (DSS)-induced animal model of colitis. <b><i>Materials and Methods:</i></b> We developed and evaluated an oral CTDS of tacrolimus (FK506) loaded pH-dependent polymeric microspheres, composed of Eudragit® S100 as a pH-sensitive polymer using the oil-in-water emulsion method. The physicochemical properties and drug release profiles of these microparticles in gastrointestinal tract (GIT) conditions were examined. A DSS-induced colitis rat model was used to evaluate the potential remedial and in vivo distribution of microspheres. <b><i>Results:</i></b> The pH-microspheres prevented a burst drug release in acidic pH conditions and showed sustained release at a colonic pH. The in vivo distribution study in the rat GIT demonstrated that pH-microspheres were successfully delivered to the inflamed colon. Moreover, it also demonstrated a significant decrease of disease activity and expression of proinflammatory cytokines, such as tumor necrosis factor α, interleukin-1β (IL-1β), and IL-6, and minimized the histological and morphometric changes. <b><i>Conclusion:</i></b> The results confirmed the efficacy of tacrolimus (FK506) CTDs in the management of DSS-induced colitis.

scholarly journals One-pot synthesis of biodegradable polydopamine-doped mesoporous silica nanocomposites (PMSNs) as pH-sensitive targeting drug nanocarriers for synergistic chemo-photothermal therapy

RSC Advances ◽  
2018 ◽  
Vol 8 (65) ◽  
pp. 37433-37440 ◽  
Author(s):  
Huicong Zhang ◽  
Xuandong Wang ◽  
Peiyuan Wang ◽  
Rong Liu ◽  
Xuemei Hou ◽  
...  
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Photothermal Therapy ◽  
Ph Sensitive ◽  
Ph Responsive ◽  
One Pot ◽  
Silica Nanocomposites ◽  
One Pot Synthesis ◽  
Drug Nanocarriers

Polydopamine-doped mesoporous silica nanocomposites (PMSNs) were controllably synthesized by a one-pot approach. They were demonstrated to be good biodegradability, pH-responsive drug release and targeting synergistic chemo-photothermal therapy.

scholarly journals Synthesis, Principles, and Properties of Magnetite Nanoparticles for In Vivo Imaging Applications—A Review

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 601 ◽  
Author(s):  
Wallyn ◽  
Anton ◽  
Vandamme
Keyword(s):  
Iron Oxide ◽  
Targeted Delivery ◽  
Biomedical Applications ◽  
Colloidal Particles ◽  
Chemical Properties ◽  
Local Drug Delivery ◽  
Physical And Chemical ◽  
Immense Potential ◽  
Drug Nanocarriers

The current nanotechnology era is marked by the emergence of various magnetic inorganic nanometer-sized colloidal particles. These have been extensively applied and hold an immense potential in biomedical applications including, for example, cancer therapy, drug nanocarriers (NCs), or in targeted delivery systems and diagnosis involving two guided-nanoparticles (NPs) as nanoprobes and contrast agents. Considerable efforts have been devoted to designing iron oxide NPs (IONPs) due to their superparamagnetic (SPM) behavior (SPM IONPs or SPIONs) and their large surface-to-volume area allowing more biocompatibility, stealth, and easy bonding to natural biomolecules thanks to grafted ligands, selective-site moieties, and/or organic and inorganic corona shells. Such nanomagnets with adjustable architecture have been the topic of significant progresses since modular designs enable SPIONs to carry out several functions simultaneously such as local drug delivery with real-time monitoring and imaging of the targeted area. Syntheses of SPIONs and adjustments of their physical and chemical properties have been achieved and paved novel routes for a safe use of those tailored magnetic ferrous nanomaterials. Herein we will emphasis a basic notion about NPs magnetism in order to have a better understanding of SPION assets for biomedical applications, then we mainly focus on magnetite iron oxide owing to its outstanding magnetic properties. The general methods of preparation and typical characteristics of magnetite are reviewed, as well as the major biomedical applications of magnetite.

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