PEG-conjugated pyrrole-based polymers: one-pot multicomponent synthesis and self-assembly into soft nanoparticles for drug delivery

2019 ◽  
Vol 55 (66) ◽  
pp. 9829-9832 ◽  
Author(s):  
Alexandre Moquin ◽  
Ramez Hanna ◽  
Tongyue Liang ◽  
Huseyin Erguven ◽  
Evan Rizzel Gran ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Self Assembly ◽  
Drug Loading ◽  
Easy Access ◽  
Multicomponent Synthesis ◽  
One Pot ◽  
Soft Nanoparticles

A simple one-pot methodology provides easy access to amphiphilic PEG–pyrrole backbone polymers, which self-assemble into soft nanoparticles enabling efficient drug loading/sustained release and can be detected inside cells.

scholarly journals Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 904
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Xiaowei Dong
Keyword(s):  
Sustained Release ◽  
Trough Concentration ◽  
Self Assembly ◽  
Subcutaneous Injection ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

Multivesicular liposome: A lipid-based drug delivery system for efficient drug delivery

2021 ◽  
Vol 27 ◽  
Author(s):  
Bapi Gorain ◽  
Bandar E. Al-Dhubiab ◽  
Anroop Nair ◽  
Prashant Kesharwani ◽  
Manisha Pandey ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Therapeutic Agents ◽  
Laboratory Research ◽  
Efficacy And Safety ◽  
Liposomal Delivery ◽  
Proteins And Peptides

: The advancement of delivery tools for therapeutic agents has brought several novel formulations with increased drug loading, sustained release, targeted delivery, and prolonged efficacy. Amongst the several novel delivery approaches, multivesicular liposome has gained potential interest because this delivery system possesses the above advantages. In addition, this multivesicular liposomal delivery prevents degradation of the entrapped drug within the physiological environment while administered. The special structure of the vesicles allowed successful entrapment of hydrophobic and hydrophilic therapeutic agents, including proteins and peptides. Furthermore, this novel formulation could maintain the desired drug concentration in the plasma for a prolonged period, which helps to reduce the dosing frequencies, improve bioavailability, and safety. This tool could also provide stability of the formulation, and finally gaining patient compliance. Several multivesicular liposomes received approval for clinical research, while others are at different stages of laboratory research. In this review, we have focused on the preparation of multivesicular liposomes along with their application in different ailments for the improvement of the performance of the entrapped drug. Moreover, the challenges of delivering multivesicular vesicles have also been emphasized. Overall, it could be inferred that multivesicular liposomal delivery is a novel platform of advanced drug delivery with improved efficacy and safety.

scholarly journals Thermosensitive Chitosan Hydrogels Containing Polymeric Microspheres for Vaginal Drug Delivery

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
Author(s):  
Ting-Ting Yang ◽  
Yuan-Zheng Cheng ◽  
Meng Qin ◽  
Yong-Hong Wang ◽  
Hong-Li Yu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Delivery System ◽  
Drug Loading ◽  
Great Promise ◽  
Burst Release ◽  
Bletilla Striata ◽  
Vaginal Drug Delivery ◽  
Thermosensitive Hydrogels

Thermosensitive hydrogels have increasingly received considerable attention for local drug delivery based on many advantages. However, burst release of drugs is becoming a critical challenge when the hydrogels are employed. Microspheres- (MS-) loaded thermosensitive hydrogels were thus fabricated to address this limitation. Employing an orthogonal design, the spray-dried operations of tenofovir (TFV)/Bletilla striata polysaccharide (BSP)/chitosan (CTS) MS were optimized according to the drug loading (DL). The physicochemical properties of the optimal MS (MS F) were characterized. Depending on the gelation temperature and gelating time, the optimal CTS-sodium alginate- (SA-) α,β-glycerophosphate (GP) (CTS-SA-GP) hydrogel was obtained. Observed by scanning electron microscope (SEM), TFV/BSP/CTS MS were successfully encapsulated in CTS-SA-GP. In vitro releasing demonstrated that MS F-CTS-SA-GP retained desirable in vitro sustained-release characteristics as a vaginal delivery system. Bioadhesion measurement showed that MS-CTS-SA-GP exhibited the highest mucoadhesive strength. Collectively, MS-CTS-SA-GP holds great promise for topical applications as a sustained-release vaginal drug delivery system.

Supramolecular micellar drug delivery system based on multi-arm block copolymer for highly effective encapsulation and sustained-release chemotherapy

2019 ◽  
Vol 7 (37) ◽  
pp. 5677-5687 ◽  
Author(s):  
Li Zhang ◽  
Dongjian Shi ◽  
Chunling Shi ◽  
Tatsuo Kaneko ◽  
Mingqing Chen
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
High Drug ◽  
Release Drug ◽  
Drug Loading Efficiency ◽  
High Drug Loading

A novel multi-arm polyphosphoester-based nanomaterial provides high drug loading efficiency and sustained-release drug delivery for effective chemotherapy.

scholarly journals One-Pot Method for Preparation of Magnetic Multi-Core Nanocarriers for Drug Delivery

Materials ◽  
2019 ◽  
Vol 12 (3) ◽  
pp. 540 ◽  
Author(s):  
Črt Dragar ◽  
Tanja Potrč ◽  
Sebastjan Nemec ◽  
Robert Roškar ◽  
Stane Pajk ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Aqueous Phase ◽  
Colloidal Stability ◽  
Drug Loading ◽  
Spherical Shape ◽  
Surfactant Solution ◽  
Time Frame ◽  
One Pot ◽  
Magnetic Nanocarriers

The development of various magnetically-responsive nanostructures is of great importance in biomedicine. The controlled assembly of many small superparamagnetic nanocrystals into large multi-core clusters is needed for effective magnetic drug delivery. Here, we present a novel one-pot method for the preparation of multi-core clusters for drug delivery (i.e., magnetic nanocarriers). The method is based on hot homogenization of a hydrophobic phase containing a nonpolar surfactant into an aqueous phase, using ultrasonication. The solvent-free hydrophobic phase that contained tetradecan-1-ol, γ-Fe2O3 nanocrystals, orlistat, and surfactant was dispersed into a warm aqueous surfactant solution, with the formation of small droplets. Then, a pre-cooled aqueous phase was added for rapid cooling and the formation of solid magnetic nanocarriers. Two different nonpolar surfactants, polyethylene glycol dodecyl ether (B4) and our own N1,N1-dimethyl-N2-(tricosan-12-yl)ethane-1,2-diamine (SP11), were investigated for the preparation of MC-B4 and MC-SP11 magnetic nanocarriers, respectively. The nanocarriers formed were of spherical shape, with mean hydrodynamic sizes <160 nm, good colloidal stability, and high drug loading (7.65 wt.%). The MC-B4 nanocarriers showed prolonged drug release, while no drug release was seen for the MC-SP11 nanocarriers over the same time frame. Thus, the selection of a nonpolar surfactant for preparation of magnetic nanocarriers is crucial to enable drug release from nanocarrier.

scholarly journals Development of a Layer-by-Layer Assembled Film on Hydrogel for Ocular Drug Delivery

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Pin Chen ◽  
Xin Wang ◽  
Yan Dong ◽  
Xiaohong Hu
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Ph Value ◽  
Drug Loading ◽  
Drug Carriers ◽  
Ocular Drug Delivery ◽  
Layer By Layer ◽  
Uv Spectrum ◽  
Modification Technique ◽  
Assembly Procedure

Hydrogel is a kind of attractive drug carriers because of its good biocompatibility and transparency. But traditional hydrogel showed some restrictions in its application in ocular drug delivery. A simple surface modification technique based on layer-by-layer (LbL) self-assembled multilayer for ocular drug delivery was developed in this work. Polycarboxymethyl-β-cyclodextrin (poly(CM-β-CD))/poly-l-lysine (PLL) multilayer film was designed and constructed for ocular drug delivery, sinceβ-CD showed good drug delivery property. The properties such as the contact angle and transparency varied a little with the deposition of poly(CM-β-CD)/PLL multilayer. Orfloxacin and puerarin were loaded into multilayer during the self-assembly procedure by two methods, which were tracked by the largest drug absorbance of UV spectrum. The loaded drug amount by incorporating drugs into poly(CM-β-CD) solution was larger than that by incorporating drugs into PLL solution. The loaded drug in the multilayer could gradually be released from multilayer in some period either for orfloxacin or for puerarin. The drug release behavior was influenced by drug loading method and pH value of released medium. Moreover, the balanced released drug amount by incorporating drugs into poly(CM-β-CD) solution is much smaller than that by incorporating drugs into PLL solution.

scholarly journals Development and Optimization of Floating Microspheres in Amethopterin

2021 ◽  
Vol 14 (4) ◽  
pp. 1538-1543
Author(s):  
Raghav Mishra
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Patient Compliance ◽  
Drug Loading ◽  
Practical Significance ◽  
In Vitro Dissolution ◽  
Minimal Risk ◽  
Gastric Residence Time

Due to the complexity of gastric emptying, as well as its considerable variability, the in vivo efficacy of drug delivery devices cannot be predicted. When it pertains to drugs with an absorption window in the upper small intestine, a controlled drug delivery system with a longer residence period in the stomach may be of considerable practical significance. Recent developments have shown that floating microspheres are particularly well suited for mixing sustained and delayed releases to achieve a variety of release models with a minimal risk of dumping. The aim of present investigation is to develop and analyze the floating microspheres of amethopterin, which after oral administration could increase the gastric residence time and enhance the bioavailability of the drug by sustained release and minimize the dose dependent side effects as well as improves patient compliance. Floating microspheres of ethyl cellulose, Polyvinyl alcohol and polyvinyl pyrrolidone-K90 were formulated by emulsification solvent evaporation technique. The various parameters of prepared microspheres were studied for SEM, flow properties, buoyancy, yield, percent drug loading, in vitro dissolution studies, stability in different pH and FTIR studies. Microspheres prepared with different concentrations of polymers were spherical in shape with smooth surface. The size of microspheres was in range of 256.02 µm and 362.84 µm. Good drug entrapment and buoyancy were observed for formulation F2. The in vitro drug release after 6h was found to be in range from 58.15% to 96.28%. It was established that the newly created floating microspheres of Amethopterin provide an appropriate and practical solution for the sustained release of medication over a longer period of time, resulting in increased oral bioavailability, effectiveness, as well as better patient compliance.

scholarly journals Miktoarm Star Polymers: Branched Architectures in Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 827 ◽  
Author(s):  
Victor Lotocki ◽  
Ashok Kakkar
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Therapeutic Interventions ◽  
Structure Property ◽  
Sustained Drug Release ◽  
Amphiphilic Macromolecules ◽  
Miktoarm Star ◽  
Core Junction

Delivering active pharmaceutical agents to disease sites using soft polymeric nanoparticles continues to be a topical area of research. It is becoming increasingly evident that the composition of amphiphilic macromolecules plays a significant role in developing efficient nanoformulations. Branched architectures with asymmetric polymeric arms emanating from a central core junction have provided a pivotal venue to tailor their key parameters. The build-up of miktoarm stars offers vast polymer arm tunability, aiding in the development of macromolecules with adjustable properties, and allows facile inclusion of endogenous stimulus-responsive entities. Miktoarm star-based micelles have been demonstrated to exhibit denser coronae, very low critical micelle concentrations, high drug loading contents, and sustained drug release profiles. With significant advances in chemical methodologies, synthetic articulation of miktoarm polymer architecture, and determination of their structure-property relationships, are now becoming streamlined. This is helping advance their implementation into formulating efficient therapeutic interventions. This review brings into focus the important discoveries in the syntheses of miktoarm stars of varied compositions, their aqueous self-assembly, and contributions their formulations are making in advancing the field of drug delivery.

Physicochemical and Drug Delivery Aspects of Lipid-Based Liquid Crystalline Nanoparticles: A Case Study of Intravenously Administered Propofol

2006 ◽  
Vol 6 (9) ◽  
pp. 3017-3024 ◽  
Author(s):  
Markus Johnsson ◽  
Justas Barauskas ◽  
Andreas Norlin ◽  
Fredrik Tiberg
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Liquid Crystalline ◽  
Drug Loading ◽  
Drug Substances ◽  
Physicochemical Features ◽  
Liquid Crystalline Nanoparticles ◽  
Effect Duration

Liquid crystalline nanoparticles (LCNP) formed through lipid self-assembly have a range of attractive properties as in vivo drug delivery carriers. In particular they offer: a wide solubilization spectrum, and consequently high drug payloads; effective encapsulation; stabilization and protection of sensitive drug substances. Here we present basic physicochemical features of non-lamellar LCNP systems with a focus on intravenous drug applications. This is exemplified by the formulation properties and in vivo behavior using the drug substance propofol; a well-known anesthetic agent currently used in clinical practice in the form of a stable emulsion. In order to appraise the drug delivery features of the LCNP system the current study was carried out with a marketed propofol emulsion product as reference. In this comparison the propofol-LCNP formulation shows several useful features including: higher drug-loading capacity, lower fat-load, excellent stability, modified pharmacokinetics, and an indication of increased effect duration.

Paclitaxel-tyroserleutide Conjugates Self-assembly into Nanocarrier for Drug Delivery

2019 ◽  
Vol 16 (8) ◽  
pp. 882-891
Author(s):  
Yongjia Liu ◽  
Leilei Shi ◽  
Bangshang Zhu ◽  
Yue Su ◽  
Hui Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Water Solubility ◽  
Drug Carrier ◽  
Drug Loading ◽  
Cancer Therapeutics ◽  
Drug Carriers ◽  
Pharmacokinetic Studies ◽  
Assembly Method

Background: The drug-drug self-assembly was considered as a simple and efficient approach to prepare high drug loading nano-drug carriers and present new opportunities for cancer therapeutics. The strategy of PTX amphiphiles preparation would be a possible way to solve the poor water solubility of PTX. Methods: The PTX-YSL conjugate were synthesized and characterized. The PTX-YSL nanocarriers was prepared by a simple self-assembly method. In vitro cell studies and pharmacokinetic studies were evaluated for their in vitro anti-tumor activities and blood retention time. Results: The structures of PTX-YSL conjugate were confirmed by LC-MS, 1H NMR and FTIR. The size and morphology of the PTX-YSL self-assembled nanocarriers were observed with TEM and DLS. PTX-YSL nanocarriers could facilitate cellular uptake and had low cytotoxicity. PTX-YSL nanocarriers have longer blood retention for enhancing accumulation in the tumor tissues via EPR effect. Conclusion: This drug delivery system formed by PTX-YSL conjugates constitutes a promising and effective drug carrier in cancer therapy.

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