Formation and property of HCO-10 vesicles new method to prepare HCO-10 vesicles with high entrapment efficiency

Novel pH-sensitive hybrid micelles with high entrapment efficiency were constructed to realize rapid intracellular drug release without premature release.

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Formulation And Evaluation Of Floating Microspheres Of Cefdinir

Journal of University of Shanghai for Science and Technology ◽

10.51201/jusst/21/11975 ◽

2021 ◽

Vol 23 (11) ◽

pp. 906-929

Author(s):

Jeslin. D ◽

◽

Nithya Kalyani.K ◽

Padmaja. V ◽

Suresh Kumar.P ◽

...

Keyword(s):

Drug Release ◽

Residence Time ◽

Entrapment Efficiency ◽

Sustained Drug Release ◽

Magnetic Systems ◽

Gastric Residence Time ◽

Gum Karaya ◽

High Entrapment Efficiency ◽

Full Factorial ◽

Good Flow

Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of cefdinir for the prolongation of gastric residence time. Themicrospheres were prepared byCapillary Extrusion method.A full factorial design was applied to optimize the formulation. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 12 hrs, high entrapment efficiency upto68%.Scanning electron microscopy confirmed the hollown structure with particle size in the order of190 μm. The studies revealed that increase in concentration of gum Karaya increased the drug release from the floating microspheres.

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Intratracheally Inhalable Nifedipine-Loaded Chitosan-PLGA Nanocomposites as a Promising Nanoplatform for Lung Targeting: Snowballed Protection via Regulation of TGF-β/β-Catenin Pathway in Bleomycin-Induced Pulmonary Fibrosis

Pharmaceuticals ◽

10.3390/ph14121225 ◽

2021 ◽

Vol 14 (12) ◽

pp. 1225

Author(s):

Mohammed H. Elkomy ◽

Rasha A. Khallaf ◽

Mohamed O. Mahmoud ◽

Raghda R. S. Hussein ◽

Asmaa M. El-Kalaawy ◽

...

Keyword(s):

Oxidative Stress ◽

Pulmonary Fibrosis ◽

Intratracheal Instillation ◽

Entrapment Efficiency ◽

Pharmacokinetic Studies ◽

Channel Blockers ◽

Systemic Bioavailability ◽

High Entrapment Efficiency ◽

And Oxidative Stress

Pulmonary fibrosis is a serious ailment that may progress to lung remodeling and demolition, where the key participants in its incidence are fibroblasts responding to growth factors and cellular calcium swinging. Calcium channel blockers, like nifedipine (NFD), may represent auspicious agents in pulmonary fibrosis treatment. Unfortunately, NFD bears complicated pharmacodynamics and a diminished systemic bioavailability. Thus, the current study aimed to develop a novel, non-invasive nanoplatform for NFD for direct/effective pulmonary targeting via intratracheal instillation. A modified solvent emulsification–evaporation method was adopted for the fabrication of NFD-nanocomposites, integrating poly(D,L-lactide-co-glycolide) (PLGA), chitosan (CTS), and polyvinyl alcohol, and optimized for different physiochemical properties according to the 32 full factorial design. Additionally, the aerodynamic behavior of the nanocomposites was scrutinized through cascade impaction. Moreover, the pharmacokinetic investigations were conducted in rats. Furthermore, the optimum formulation was tested in bleomycin-induced pulmonary fibrosis in rats, wherein fibrotic and oxidative stress parameters were measured. The optimum nanocomposites disclosed a nanosized spherical morphology (226.46 nm), a high entrapment efficiency (61.81%) and a sustained release profile over 24 h (50.4%). As well, it displayed a boosted in vitro lung deposition performance with a mass median aerodynamic diameter of 1.12 µm. Pharmacokinetic studies manifested snowballed bioavailability of the optimal nanocomposites by 3.68- and 2.36-fold compared to both the oral and intratracheal suspensions, respectively. The intratracheal nanocomposites revealed a significant reduction in lung fibrotic and oxidative stress markers notably analogous to normal control besides repairing abnormality in TGF-β/β-catenin pathway. Our results conferred a compelling proof-of-principle that NFD-CTS-PLGA nanocomposites can function as a promising nanoparadigm for pulmonary fibrosis management.

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Preparation and Characterization of Liposomal Everolimus by Thin-Film Hydration Technique

Advances in Polymer Technology ◽

10.1155/2020/5462949 ◽

2020 ◽

Vol 2020 ◽

pp. 1-9

Author(s):

Gabriela Torres-Flores ◽

Azucena Gonzalez-Horta ◽

Yadira I. Vega-Cantu ◽

Ciro Rodriguez ◽

Aida Rodriguez-Garcia

Keyword(s):

Thin Film ◽

Encapsulation Efficiency ◽

Entrapment Efficiency ◽

Hydrophobic Drug ◽

Promising Alternative ◽

Stent Restenosis ◽

Coronary Stent Implantation ◽

High Entrapment Efficiency ◽

In Stent Restenosis

In 10% to 40% of the cases of coronary stent implantation, patients face in-stent restenosis due to an inflammatory response, which induces artery thickening. Everolimus, a drug that inhibits growth factor-stimulated cell proliferation of endothelial cells, represents a promising alternative to prevent in-stent restenosis. In this study, everolimus was encapsulated by a film hydration technique in liposomes by using phosphatidylcholine and cholesterol at different ratios. As the ratio of cholesterol increases, it modulates the rigidity of the structure which can affect the encapsulation efficiency of the drug due to steric hindrance. Moreover, various lipid : drug ratios were tested, and it was found that as the lipid : drug ratio increases, the encapsulation efficiency also increases. This behavior is observed because everolimus is a hydrophobic drug; therefore, if the lipidic region increases, more drug can be entrapped into the liposomes. In addition, stability of the encapsulated drug was tested for 4 weeks at 4°C. Our results demonstrate that it is possible to prepare liposomal everolimus by film hydration technique followed by extrusion with high entrapment efficiency as a viable drug delivery system.

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Pharmacosomes: An approach to improve biopharmaceutical properties of drugs basic considerations in development

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00779 ◽

2021 ◽

pp. 4485-4490

Author(s):

Popat Kumbhar ◽

Tejaswini Shinde ◽

Tejaswini Jadhav ◽

Tejas Gavade ◽

Rushikesh Sorate ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Drug Stability ◽

Entrapment Efficiency ◽

Delivery Systems ◽

Controlled Delivery ◽

State Measurement ◽

High Entrapment Efficiency ◽

Biopharmaceutical Properties

Vesicular drug delivery systems including niososmes, liposomes, pharmacosomes, transferosomes, electrosomes, ethosomes, etc have been widely accepted for controlled delivery of the drug. Amongst, all these drug delivery systems pharmacosomes are gaining more attention of the researchers due to several benefits such as high entrapment efficiency, improved biopharmaceutical properties, and pharmacokinetic performance, no leakage or loss of drug, stability, etc. Pharmacosomes are amphiphilic phospholipid complexes of drugs having active hydrogen that bind to phospholipids and self-assembled into vesicles in an aqueous medium. Both hydrophilic and lipophilic drugs have been formulated into pharmacosomes that caused improved solubility and permeability of drugs. Pharmacosomes are prepared by using various techniques such as hand shaking method, ether injection, solvent evaporation method, supercritical fluid approach, etc and are characterized for prodrug confirmation, surface morphology, crystal state measurement, in vitro drug release, and stability, etc. Despite wide research and highly encouraging results in the preclinical studies, translation of these nanomedicines from laboratory to market has been very limited. The main aim of this review is to describe comprehensively the potential of pharmacosomes as a vesicular drug delivery system focusing mainly on their conventional and advanced methods of preparation, different characterization techniques, and their applications in the delivery of different types of drugs with improved biopharmaceutical properties and pharmacokinetic performance.

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Preparation and Evaluation of Intraperitoneal Long-Acting Oxaliplatin-Loaded Multi-Vesicular Liposomal Depot for Colorectal Cancer Treatment

Pharmaceutics ◽

10.3390/pharmaceutics12080736 ◽

2020 ◽

Vol 12 (8) ◽

pp. 736

Author(s):

Sharif Md Abuzar ◽

Eun Jung Park ◽

Yeji Seo ◽

Juseung Lee ◽

Seung Hyuk Baik ◽

...

Keyword(s):

Colorectal Cancer ◽

Drug Release ◽

Entrapment Efficiency ◽

Lag Phase ◽

Burst Release ◽

Sustained Drug Release ◽

Long Acting ◽

High Entrapment Efficiency

Colorectal cancer with peritoneal metastasis has a poor prognosis because of inadequate responses to systemic chemotherapy. Cytoreductive surgery followed by intraperitoneal (IP) chemotherapy using oxaliplatin has attracted attention; however, the short half-life of oxaliplatin and its rapid clearance from the peritoneal cavity limit its clinical application. Here, a multivesicular liposomal (MVL) depot of oxaliplatin was prepared for IP administration, with an expected prolonged effect. After optimization, a combination of phospholipids, cholesterol, and triolein was used based on its ability to produce MVL depots of monomodal size distribution (1–20 µm; span 1.99) with high entrapment efficiency (EE) (92.16% ± 2.17%). An initial burst release followed by a long lag phase of drug release was observed for the MVL depots system in vitro. An in vivo pharmacokinetic study mimicking the early postoperative IP chemotherapy regimen in rats showed significantly improved bioavailability, and the mean residence time of oxaliplatin after IP administration revealed that slow and continuous erosion of the MVL particles yielded a sustained drug release. Thus, oxaliplatin-loaded MVL depots presented in this study have potential for use in the treatment of colorectal cancer.

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Partial Surface Modification of Low Generation Polyamidoamine Dendrimers: Gaining Insight into their Potential for Improved Carboplatin Delivery

Biomolecules ◽

10.3390/biom9060214 ◽

2019 ◽

Vol 9 (6) ◽

pp. 214 ◽

Cited By ~ 8

Author(s):

Nguyen ◽

Bach ◽

Nguyen Tran ◽

Cao ◽

Nguyen ◽

...

Keyword(s):

Renal Clearance ◽

Size Range ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Efficient Delivery ◽

Methoxypolyethylene Glycol ◽

Potential Applications ◽

High Entrapment Efficiency ◽

Surface Modified

Carboplatin (CAR) is a second generation platinum-based compound emerging as one of the most widely used anticancer drugs to treat a variety of tumors. In an attempt to address its dose-limiting toxicity and fast renal clearance, several delivery systems (DDSs) have been developed for CAR. However, unsuitable size range and low loading capacity may limit their potential applications. In this study, PAMAM G3.0 dendrimer was prepared and partially surface modified with methoxypolyethylene glycol (mPEG) for the delivery of CAR. The CAR/PAMAM G3.0@mPEG was successfully obtained with a desirable size range and high entrapment efficiency, improving the limitations of previous CAR-loaded DDSs. Cytocompatibility of PAMAM G3.0@mPEG was also examined, indicating that the system could be safely used. Notably, an in vitro release test and cell viability assays against HeLa, A549, and MCF7 cell lines indicated that CAR/PAMAM G3.0@mPEG could provide a sustained release of CAR while fully retaining its bioactivity to suppress the proliferation of cancer cells. These obtained results provide insights into the potential of PAMAM G3.0@mPEG dendrimer as an efficient delivery system for the delivery of a drug that has strong side effects and fast renal clearance like CAR, which could be a promising approach for cancer treatment.

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