scholarly journals Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

Polymers ◽  
2021 ◽  
Vol 13 (23) ◽  
pp. 4189
Author(s):  
Sergey K. Filippov ◽  
Ramil R. Khusnutdinov ◽  
Wali Inham ◽  
Chang Liu ◽  
Dmitry O. Nikitin ◽  
...  
Keyword(s):  
Drug Loading ◽  
Amorphous State ◽  
Hybrid Nanoparticles ◽  
Titration Calorimetry ◽  
Polymeric Surfactant ◽  
Striking Difference ◽  
Scanning Calorimetry ◽  
Onset Of Action ◽  
Eudragit L100 ◽  
Loading Efficiency

The choice of drug delivery carrier is of paramount importance for the fate of a drug in a human body. In this study, we have prepared the hybrid nanoparticles composed of FDA-approved Eudragit L100-55 copolymer and polymeric surfactant Brij98 to load haloperidol—an antipsychotic hydrophobic drug used to treat schizophrenia and many other disorders. This platform shows good drug-loading efficiency and stability in comparison to the widely applied platforms of mesoporous silica (MSN) and a metal–organic framework (MOF). ZIF8, a biocompatible MOF, failed to encapsulate haloperidol, whereas MSN only showed limited encapsulation ability. Isothermal titration calorimetry showed that haloperidol has low binding with the surface of ZIF8 and MSN in comparison to Eudragit L100-55/Brij98, thus elucidating the striking difference in haloperidol loading. With further optimization, the haloperidol loading efficiency could reach up to 40% in the hybrid Eudragit L100-55/Brij98 nanoparticles with high stability over several months. Differential scanning calorimetry studies indicate that the encapsulated haloperidol stays in an amorphous state inside the Eudragit L100-55/Brij98 nanoparticles. Using a catalepsy and open field animal tests, we proved the prolongation of haloperidol release in vivo, resulting in later onset of action compared to the free drug.

Novel Self-Assembled Polycaprolactone–Lipid Hybrid Nanoparticles Enhance the Antibacterial Activity of Ciprofloxacin

2020 ◽  
Vol 25 (6) ◽  
pp. 598-607
Author(s):  
Mustafa E. Omer ◽  
Majed Halwani ◽  
Rayan M. Alenazi ◽  
Omar Alharbi ◽  
Shokran Aljihani ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Drug Loading ◽  
In Vitro Release ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Hybrid Nanoparticles ◽  
Diffusion Method ◽  
Prolonged Release ◽  
Scanning Calorimetry

Ciprofloxacin (CIP), a widely used antibiotic, is a poor biopharmaceutical resulting in low bioavailability. We optimized a CIP polymer–lipid hybrid nanoparticle (CIP-PLN) delivery system to enhance its biopharmaceutical attributes and the overall therapeutic performance. CIP-PLN formulations were prepared by a direct emulsification–solvent–evaporation method. Varying the type and ratio of lipid was tried to optimize a CIP-PLN formulation. All the prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, physical stability, and drug entrapment efficiency. The drug in vitro release profile was also studied. Antibacterial activities were tested by the agar diffusion method for all CIP-PLN formulations against an Escherichia coli clinical bacterial isolate (EC04). CIP-PLN formulations showed average sizes in the range of 133.9 ± 1.7 nm to 217.1 ± 0.8 nm, exhibiting high size uniformity as indicated by polydispersity indices lower than 0.25. The entrapment efficiency was close to 80% for all formulations. The differential scanning calorimetry (DSC) thermograms indicated the existence of CIP in the amorphous state in all PLN formulations. Fourier transform infrared spectra indicated deep incorporation of molecular CIP within the polymer matrix. The release profile of CIP from PLN formulas showed a uniform prolonged drug profile, extended for a week from most formulations with a zero-order kinetics. The antibacterial activity of CIP-PLN formulations showed significantly higher antibacterial activity only with F4 containing lecithin as the lipid component. In conclusion, we successfully optimized a CIP-PLN formulation with a low nanoparticle size in a close range, high percentage of entrapment efficiency and drug loading, uniform prolonged release rate, and higher antibacterial activity against the EC04 clinical isolate.

scholarly journals Oral Drug Delivery Systems Based on Ordered Mesoporous Silica Nanoparticles for Modulating the Release of Aprepitant

2021 ◽  
Vol 22 (4) ◽  
pp. 1896
Author(s):  
Theodora Christoforidou ◽  
Dimitra Giasafaki ◽  
Eleftherios G. Andriotis ◽  
Nikolaos Bouropoulos ◽  
Nikoleta F. Theodoroula ◽  
...  
Keyword(s):  
Silica Nanoparticles ◽  
Oral Drug Delivery ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Active Agent ◽  
Amorphous State ◽  
Diffusion Method ◽  
Oral Drug ◽  
Scanning Calorimetry ◽  
Ordered Mesoporous

Two different types of ordered mesoporous nanoparticles, namely MCM-41 and MCM-48, with similar pore sizes but different pore connectivity, were loaded with aprepitant via a passive diffusion method. The percentage of the loaded active agent, along with the encapsulation efficiency, was evaluated using High-performance Liquid Chromatography (HPLC) analysis complemented by Thermogravimetric Analysis (TGA). The determination of the pore properties of the mesoporous particles before and after the drug loading revealed the presence of confined aprepitant in the pore structure of the particles, while Powder X-ray Diffractometry(pXRD), Differential Scanning Calorimetry (DSC), and FTIR experiments indicated that the drug is in an amorphous state. The release profiles of the drug from the two different mesoporous materials were studied in various release media and revealed an aprepitant release up to 45% when sink conditions are applied. The cytocompatibility of the silica nanoparticles was assessed in Caco-2 cell monolayers, in the presence and absence of the active agent, suggesting that they can be used as carriers of aprepitant without presenting any toxicity in vitro.

scholarly journals CHARACTERIZATION OF DRUGS ENCAPSULATED INTO MESOPOROUS SILICA

2019 ◽  
pp. 7-11
Author(s):  
ARIF BUDIMAN
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Molecular State ◽  
Water Soluble ◽  
Crystal Nucleation ◽  
Formulation Development ◽  
Scanning Calorimetry

Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.

scholarly journals Enhanced Dissolution Efficiency of Tamoxifen Combined with Methacrylate Copolymers in Amorphous Solid Dispersions

Crystals ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 1046
Author(s):  
Dayanne T. C. da Silva ◽  
Daniela Nadvorny ◽  
Lucas J. de A. Danda ◽  
Amanda C. Q. de M. Vieira ◽  
Patricia Severino ◽  
...  
Keyword(s):  
Drug Loading ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Amorphous Solid ◽  
Physical Mixture ◽  
Polymer Mixture ◽  
Scanning Calorimetry ◽  
Amorphous Solid Dispersions ◽  
Acrylate Copolymer ◽  
Poorly Soluble

Amorphous solid dispersions (SDs) containing poorly soluble tamoxifen dispersed in a meth(acrylate) copolymer combination were proposed as a controlled release system. The objective of this work was to investigate the characteristics and performance of the tamoxifen–polymer mixture and evaluate the changes in functionality through a supersaturating dissolution study condition while comparing it to a physical mixture at a fixed drug-loading proportion. Two polymers, Eudragit® L 100 and Eudragit® RL 100, were used to prepare SDs with a 1:1 polymer ratio, containing 10%, 20%, or 30% (wt/wt%) of tamoxifen, by the solvent evaporation method. A physical mixture containing 30% of tamoxifen was also prepared for comparison. SDs were characterized by X-ray diffraction, Fourier-transform infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. Dissolution tests were conducted under non-sink conditions to verify the occurrence of drug recrystallization upon its release. Solid-state characterizations confirmed that the drug was in the amorphous state within the polymeric matrix. Tamoxifen release in an acidic medium was mainly affected by the increase in drug concentration caused by the possible loss of interactions that characterize the main polymer functionalities. At pH 7.4, supersaturation was slowly achieved while also contributing to the increase in the kinetic solubility of the drug. The physical mixture demonstrated the best overall performance, suggesting that the polymeric interactions may have negatively affected the drug release. The combination of polymers in the composing SD proved to be a promising strategy to tailor the delivery of poorly soluble drugs. Our study highlights important information on the behavior of tamoxifen as a poorly soluble drug in supersaturating dissolution conditions while released from SD systems.

scholarly journals Diazepam Loaded Solid Lipid Nanoparticles: In Vitro and in Vivo Evaluations

2020 ◽  
Author(s):  
Sara Faghihi ◽  
Mohammad Reza Awadi ◽  
Seyyedeh Elaheh Mousavi ◽  
Seyyed Mahdi Rezayat Sorkhabadi ◽  
Mandana Karboni ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Spherical Shape ◽  
Lipid Nanoparticles ◽  
Male Rats ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Loading Efficiency

Purpose: To overcome side effects of repetitive administration of Diazepam (Dzp) besides gaining benefits from sustaining release (SR) of the drug, which contributes to patient compliance, we concentrated on designing and preparing Dzp Solid Lipid Nanoparticles (SLNs). Methods: Using cholesterol (CHOL), stearic acid (SA) and glycerol monostearate (GMS), SLNs were prepared by high shear homogenization technique coupled with sonication. Polysorbate 80 (Tween 80) was used as a nonionic surfactant. After modification of prepared SLNs, particle size, zeta potential, drug-loading efficiency, morphology and scanning calorimetry as well as release studies were conducted. To increase the stability of desired particles, freeze-drying by cryoprotectant was carried out. In the final stage, In-vivo study was performed by oral (PO) and intraperitoneal (IP) administration to Wistar male rats. Results: Results indicated that optimized prepared particles were in average 150 nm diameter in spherical shape with 79.06 % loading efficiency and release of more than 85% of loaded drug in 24 hours. In-vivo investigations also illustrated differences in blood distribution of Dzp after loading this drug into SLNs. Conclusion: Based on the findings, it seems that drug delivery using SLNs could be an opportunity for solving complications of Dzp therapy in future.

Present trends in the encapsulation of anticancer drugs

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Xavier Montané ◽  
Karolina Matulewicz ◽  
Karolina Balik ◽  
Paulina Modrakowska ◽  
Marcin Łuczak ◽  
...  
Keyword(s):  
Carbon Nanotubes ◽  
Drug Toxicity ◽  
Recent Progress ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
The Body ◽  
Inorganic Nanoparticles ◽  
Hybrid Nanoparticles ◽  
Traditional Medicines ◽  
Low Solubility

Abstract Different nanomedicine devices that were developed during the recent years can be suitable candidates for their application in the treatment of various deadly diseases such as cancer. From all the explored devices, the nanoencapsulation of several anticancer medicines is a very promising approach to overcome some drawbacks of traditional medicines: administered dose of the drugs, drug toxicity, low solubility of drugs, uncontrolled drug delivery, resistance offered by the physiological barriers in the body to drugs, among others. In this chapter, the most important and recent progress in the encapsulation of anticancer medicines is examined: methods of preparation of distinct nanoparticles (inorganic nanoparticles, dendrimers, biopolymeric nanoparticles, polymeric micelles, liposomes, polymersomes, carbon nanotubes, quantum dots, and hybrid nanoparticles), drug loading and drug release mechanisms. Furthermore, the possible applications in cancer prevention, diagnosis, and cancer therapy of some of these nanoparticles have been highlighted.

scholarly journals A review of nanotechnology with an emphasis on Nanoplex

2015 ◽  
Vol 51 (2) ◽  
pp. 255-263
Author(s):  
Rupali Nanasaheb Kadam ◽  
Raosaheb Sopanrao Shendge ◽  
Vishal Vijay Pande
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Loading ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Conventional Drug ◽  
Anionic Drugs ◽  
Oppositely Charged ◽  
The Brain

<p>The use of nanotechnology based on the development and fabrication of nanostructures is one approach that has been employed to overcome the challenges involved with conventional drug delivery systems. Formulating Nanoplex is the new trend in nanotechnology. A nanoplex is a complex formed by a drug nanoparticle with an oppositely charged polyelectrolyte. Both cationic and anionic drugs form complexes with oppositely charged polyelectrolytes. Compared with other nanostructures, the yield of Nanoplex is greater and the complexation efficiency is better. Nanoplex are also easier to prepare. Nanoplex formulation is characterized through the production yield, complexation efficiency, drug loading, particle size and zeta potential using scanning electron microscopy, differential scanning calorimetry, X-ray diffraction and dialysis studies. Nanoplex have wide-ranging applications in different fields such as cancer therapy, gene drug delivery, drug delivery to the brain and protein and peptide drug delivery.</p>

scholarly journals The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 455
Author(s):  
Emilia Szymańska ◽  
Katarzyna Woś-Latosi ◽  
Julia Jacyna ◽  
Magdalena Dąbrowska ◽  
Joanna Potaś ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Drug Loading ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Complex Nature ◽  
Prolonged Release ◽  
Scanning Calorimetry ◽  
Burst Effect ◽  
The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

scholarly journals Tailoring Atomoxetine Release Rate from DLP 3D-Printed Tablets Using Artificial Neural Networks: Influence of Tablet Thickness and Drug Loading

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 111
Author(s):  
Gordana Stanojević ◽  
Djordje Medarević ◽  
Ivana Adamov ◽  
Nikola Pešić ◽  
Jovana Kovačević ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Release Rate ◽  
Drug Loading ◽  
Prolonged Release ◽  
Cylindrical Shape ◽  
Poly Ethylene Glycol ◽  
Scanning Calorimetry ◽  
3D Printed ◽  
Artificial Neural ◽  
Poly Ethylene

Various three-dimensional printing (3DP) technologies have been investigated so far in relation to their potential to produce customizable medicines and medical devices. The aim of this study was to examine the possibility of tailoring drug release rates from immediate to prolonged release by varying the tablet thickness and the drug loading, as well as to develop artificial neural network (ANN) predictive models for atomoxetine (ATH) release rate from DLP 3D-printed tablets. Photoreactive mixtures were comprised of poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) 400 in a constant ratio of 3:1, water, photoinitiator and ATH as a model drug whose content was varied from 5% to 20% (w/w). Designed 3D models of cylindrical shape tablets were of constant diameter, but different thickness. A series of tablets with doses ranging from 2.06 mg to 37.48 mg, exhibiting immediate- and modified-release profiles were successfully fabricated, confirming the potential of this technology in manufacturing dosage forms on demand, with the possibility to adjust the dose and release behavior by varying drug loading and dimensions of tablets. DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction) and microscopic analysis showed that ATH remained in a crystalline form in tablets, while FTIR spectroscopy confirmed that no interactions occurred between ATH and polymers.

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