scholarly journals Proteinoid Nanocapsules as Drug Delivery System for Improving Antipsychotic Activity of Risperidone

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 4013
Author(s):  
Liroy Lugasi ◽  
Igor Grinberg ◽  
Rivka Sabag ◽  
Ravit Madar ◽  
Haim Einat ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Drug Loading ◽  
Continuous Phase ◽  
Drug Effectiveness ◽  
Long Term Storage ◽  
Behavioral Studies ◽  
Antipsychotic Activity ◽  
The Stability

Risperidone (RSP) is an atypical antipsychotic drug widely used to treat schizophrenia and bipolar disorder. Nanoparticles (NPs) are being developed as in vivo targeted drug delivery systems, which cross the blood-brain barrier and improve pharmacokinetics and drug effectiveness. Here, biodegradable proteinoids were synthesized by thermal step-growth polymerization from the amino acids l-glutamic acid, l-phenylalanine and l-histidine and poly (l-lactic acid). Proteinoid NPs containing RSP were then formed by self-assembly, overcoming the insolubility of the drug in water, followed by PEGylation (poly ethylene glycol (PEG) conjugation to increase the stability of the NPs in the aqueous continuous phase. These NPs are biodegradable owing to their peptide and ester moieties. They were characterized in terms of diameter, size distribution, drug loading, and long-term storage. Behavioral studies on mice found enhanced antipsychotic activity compared to free RSP.

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.

scholarly journals Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity

2020 ◽  
Vol 18 (1) ◽  
Author(s):  
L. Lugasi ◽  
I. Grinberg ◽  
S. Rudnick-Glick ◽  
E. Okun ◽  
H. Einat ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Drug Loading ◽  
Drug Efficacy ◽  
Aqueous Solubility ◽  
Antipsychotic Activity ◽  
Step Growth ◽  
Step Growth Polymerization ◽  
Drug Efficiency ◽  
Atypical Antipsychotic Medication

Abstract Background Nanoparticles (NPs) incorporating drug formulations can be used to facilitate passage through biological barriers including the blood–brain barrier (BBB) and increase drug delivery and bioavailability. Hence, NP-based administration may enhance the efficiency of current antipsychotics. Encapsulation within NPs can resolve aqueous solubility problems that not only reduce permeability through the BBB but also affect targeting. The present study describes a new drug delivery system based on proteinoid NPs to explore the possibility of improving drug efficacy. Risperidone (RSP) is a commonly used atypical antipsychotic medication, and was therefore selected for encapsulation by proteinoid NPs. Results Proteinoid polymers with high molecular weight and low polydispersity were synthesized from l-amino acids and poly-l-lactic acid (PLLA) by thermal step-growth polymerization mechanism. RSP-loaded proteinoid NPs were then prepared using a self-assembly process in the presence of RSP, followed by PEGylation. The optimal PEGylated RSP-loaded NPs were characterized in terms of diameter and size distribution, drug loading, ζ-potential, cytotoxicity, biodistribution, and psychopharmacological effects. The findings indicate significantly higher antipsychotic activity of drug-loaded proteinoid NPs compared to free RSP. Conclusions Proteinoid NPs enhance RSP delivery and may potentially increase drug efficiency by reducing dosage and side effects.

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.

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

scholarly journals Stability of Engineered Micro or Nanobubbles for Biomedical Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1089
Author(s):  
Beomjin Park ◽  
Semi Yoon ◽  
Yonghyun Choi ◽  
Jaehee Jang ◽  
Soomin Park ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Biomedical Applications ◽  
Ultrasonic Field ◽  
Nanometer Scale ◽  
Factors Affecting ◽  
The Core ◽  
Bubble Structure ◽  
The Stability ◽  
The Relationship

A micro/nanobubble (MNB) refers to a bubble structure sized in a micrometer or nanometer scale, in which the core is separated from the external environment and is normally made of gas. Recently, it has been confirmed that MNBs can be widely used in angiography, drug delivery, and treatment. Thus, MNBs are attracting attention as they are capable of constructing a new contrast agent or drug delivery system. Additionally, in order to effectively use an MNB, the method of securing its stability is also being studied. This review highlights the factors affecting the stability of an MNB and the stability of the MNB within the ultrasonic field. It also discusses the relationship between the stability of the bubble and its applicability in vivo.

Active-targeting and acid-sensitive pluronic prodrug micelles for efficiently overcoming MDR in breast cancer

2020 ◽  
Vol 8 (13) ◽  
pp. 2726-2737
Author(s):  
Cheng Xu ◽  
Jiaxi Xu ◽  
Yan Zheng ◽  
Qin Fang ◽  
Xiaodong Lv ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Drug Delivery ◽  
Self Assembly ◽  
Active Targeting

The mechanism of pluronic-based prodrug micelles self-assembly, drug delivery and anti-MDR in vivo.

scholarly journals IRONSperm: Sperm-templated soft magnetic microrobots

2020 ◽  
Vol 6 (28) ◽  
pp. eaba5855 ◽  
Author(s):  
Veronika Magdanz ◽  
Islam S. M. Khalil ◽  
Juliane Simmchen ◽  
Guilherme P. Furtado ◽  
Sumit Mohanty ◽  
...  
Keyword(s):  
Self Assembly ◽  
Drug Loading ◽  
Chemotherapeutic Agents ◽  
Single Step ◽  
Biological Entity ◽  
Sperm Cells ◽  
Soft Magnetic ◽  
Actuation Frequency ◽  
Magnetic Microrobots

We develop biohybrid magnetic microrobots by electrostatic self-assembly of nonmotile sperm cells and magnetic nanoparticles. Incorporating a biological entity into microrobots entails many functional advantages beyond shape templating, such as the facile uptake of chemotherapeutic agents to achieve targeted drug delivery. We present a single-step electrostatic self-assembly technique to fabricate IRONSperms, soft magnetic microswimmers that emulate the motion of motile sperm cells. Our experiments and theoretical predictions show that the swimming speed of IRONSperms exceeds 0.2 body length/s (6.8 ± 4.1 µm/s) at an actuation frequency of 8 Hz and precision angle of 45°. We demonstrate that the nanoparticle coating increases the acoustic impedance of the sperm cells and enables localization of clusters of IRONSperm using ultrasound feedback. We also confirm the biocompatibility and drug loading ability of these microrobots, and their promise as biocompatible, controllable, and detectable biohybrid tools for in vivo targeted therapy.

A γ-cyclodextrin-based metal–organic framework embedded with graphene quantum dots and modified with PEGMA via SI-ATRP for anticancer drug delivery and therapy

Nanoscale ◽  
2019 ◽  
Vol 11 (43) ◽  
pp. 20956-20967 ◽  
Author(s):  
Qiaojuan Jia ◽  
Zhenzhen Li ◽  
Chuanpan Guo ◽  
Xiaoyu Huang ◽  
Yingpan Song ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Metal Organic Framework ◽  
Drug Loading ◽  
Graphene Quantum Dots ◽  
Tumor Growth Inhibition ◽  
High Drug ◽  
Anticancer Drug Delivery ◽  
Metal Organic ◽  
High Drug Loading

A biocompatible γ-CD-MOF based DDS with high drug loading and full drug release was prepared and effective tumor growth inhibition was achieved in vivo.

scholarly journals FORMULATION OF NANOPARTICLES OF TELMISARTAN INCORPORATED IN CARBOXYMETHYLCHITOSAN FOR THE BETTER DRUG DELIVERY AND ENHANCED BIOAVAILABILITY

2017 ◽  
Vol 10 (9) ◽  
pp. 236
Author(s):  
Upasana Yadav ◽  
Angshuman Ray Chowdhuri ◽  
Sumanta Kumar Sahu ◽  
Nuzhat Husain ◽  
Qamar Rehman
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Water Soluble ◽  
Bioavailability Enhancement ◽  
Water Soluble Drug ◽  
Efficient Option

  Objective: In this study, we have made an attempt to the developed formulation of nanoparticles (NPs) of telmisartan (TLM) incorporated in carboxymethyl chitosan (CMCS) for the better drug delivery and enhanced bioavailability.Materials and Methods: The NPs size and morphology were investigated by high-resolution transmission electron microscopy and field emission scanning electron microscopy, respectively. The crystal structures and surface functional groups were analyzed using X-ray diffraction pattern, and Fourier transform infrared spectroscopy, respectively.Results: To increase the solubility of TLM by targeted delivery of the drug through polymeric NPs is an alternative efficient, option for increasing the solubility. TLM nanosuspension powders were successfully formulated for dissolution and bioavailability enhancement of the drug. We focused on evaluating the influence of particle size and crystalline state on the in vitro and in vivo performance of TLM.Conclusion: In summary, we have developed a new approach toward the delivery of poorly water-soluble drug TLM by CMCS NPs. The particles having a good drug loading content and drug encapsulation efficiency. The cytotoxicity of the synthesized NPs is also very less.

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.

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