scholarly journals Synthesis of Ester-linked Docetaxel-glycoside Conjugate and Its Application to Drug Delivery System using Immunoliposome Targeted with Trastuzumab

2016 ◽  
Vol 11 (11) ◽  
pp. 1934578X1601101 ◽  
Author(s):  
Hiroki Hamada ◽  
Shouta Okada ◽  
Kei Shimoda ◽  
Hatsuyuki Hamada ◽  
Noriyoshi Masuoka
Keyword(s):  
Drug Delivery ◽  
Tumor Growth ◽  
Drug Delivery System ◽  
Delivery System ◽  
Enzymatic Synthesis ◽  
Water Solubility ◽  
Effective Suppression

Chemo-enzymatic synthesis of the ester-linked monosaccharide conjugate of docetaxel, 7-glycolyldocetaxel 2″- O-β-D-galactopyranoside, was achieved by using lactase as a biocatalyst. The water-solubility and, EE and LE values for the liposome of 7-glycolyldocetaxel 2″- O-β-D-galactopyranoside were much higher than those of docetaxel. The immunoliposome containing 7-glycolyldocetaxel 2″- O-β-D-galactopyranoside showed effective suppression of tumor growth.

scholarly journals Chemo-enzymatic Synthesis of Ester-Linked Docetaxel-Glycoside Conjugate and its Drug Delivery System Using Hybrid-Bio-Nanocapsules Targeted With Trastuzumab and Cetuximab

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1985880
Author(s):  
Yuya Fujitaka ◽  
Hiroki Hamada ◽  
Hatsuyuki Hamada ◽  
Noriyoshi Masuoka ◽  
Kei Shimoda ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tumor Growth ◽  
Drug Delivery System ◽  
Delivery System ◽  
Enzymatic Synthesis ◽  
Effective Suppression ◽  
Anti Cancer ◽  
Cancer Activity

Synthesis of ester-linked glucoside conjugate of docetaxel, 7-propionyldocetaxel 3''- O-α-D-glucopyranoside, was carried out by chemo-enzymatic procedures. The EE and LE values for hybrid-bio-nanocapsules of 7-propionyldocetaxel 3''- O-α-D-glucopyranoside were much improved rather than those of docetaxel. The hybrid-bio-nanocapsules targeted with trastuzumab and cetuximab, which contained 7-propionyldocetaxel 3''- O-α-D-glucopyranoside, showed high in vivo anti-cancer activity, ie, effective suppression of tumor growth, respectively.

scholarly journals Chemo-Enzymatic Synthesis of Glycolyl-Ester-Linked Taxol-Monosaccharide Conjugate and Its Drug Delivery System Using Hepatitis B Virus Envelope L Bio-Nanocapsules

2012 ◽  
Vol 5 ◽  
pp. BCI.S9824
Author(s):  
Kei Shimoda ◽  
Manabu Hamada ◽  
Masaharu Seno ◽  
Tadakatsu Mandai ◽  
Hiroki Hamada
Keyword(s):  
Hepatocellular Carcinoma ◽  
Drug Delivery ◽  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Drug Delivery System ◽  
Delivery System ◽  
Enzymatic Synthesis ◽  
Water Solubility ◽  
Virus Envelope ◽  
B Virus

Chemo-enzymatic synthesis of glycolyl-ester-linked taxol-glucose conjugate, ie, 7-glycolyltaxol 2′- O-α-D-glucoside, was achieved by using α-glucosidase as a biocatalyst. The water-solubility of 7-glycolyltaxol 2′- O-α-D-glucoside (21 μM) was 53 fold higher than that of taxol. The hepatitis B virus envelope L particles (bio-nanocapsules) are effective for delivering 7-glycolyltaxol 2′- O-α-D-glucoside to human hepatocellular carcinoma NuE cells.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

scholarly journals A Literature Review on Self Nanoemulsifying Drug Delivery System (SNEDDS)

2021 ◽  
Vol 70 (1) ◽  
Author(s):  
Saikumar D ◽  
Leela Prasanna J
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Solubility ◽  
Solvent Molecule ◽  
Water Soluble ◽  
Statistical Experimental Design ◽  
Characterization Methods ◽  
Nano Emulsion ◽  
Pharmacologically Active

The Lipid-based drug delivery system is extensively reported within the literature for the enhancing drug solubility, permeability, and bioavailability. A considerable majority of novel pharmacologically active constituents produced in recent drug discovery programs are lipophilic and poorly soluble, posing a significant problem for pharmaceutical researchers enhancing the oral bioavailability of such drug molecules. Self-nano emulsifying drug delivery systems (SNEDDS), are the viable oil-based approaches for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, researchers have been focusing on the challenges of BCS Class II and Class IV Drugs for enhancing water Solubility of poorly water-soluble drugs. SNEDDS is a Validate method for enhancing the solubility and bioavailability of lipophilic compounds. It’s the isotropic mixture of oil, surfactant, co-surfactant molecules and it also containing co-solvent molecule. which spontaneously form oil-in-water nano emulsion of approximately 200 nm or less in size upon dilution with water under gentle stirring. It’s Drug delivery system Which possess thermodynamically and kinetically stability. The physicochemical properties, drug solubilization capacity considerably regulates the selection of the SNEDDS components. The compositions of the SNEDDS are often optimized with the assistance of phase diagrams. Further to optimize SNEDDS can be done with the help of statistical experimental design. It’s a Novel drug delivery system which is applicable for the parenteral, Ophthalmic, intranasal and cosmetic drug delivery system. And therefore, the present review describes Preparation, components, mechanism of self-Nano emulsification, biopharmaceutical aspects, characterization methods and applications of Selfnanoemulsifying drug delivery system (SNEDDS).

scholarly journals Enhanced antitumor efficacy on colon cancer using EGF functionalized PLGA nanoparticles loaded with 5-Fluorouracil and perfluorocarbon

2019 ◽  
Author(s):  
Pingping Wu ◽  
Qing Zhou ◽  
Huayun Zhu ◽  
Yan Zhuang ◽  
Jun Bao
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Tumor Growth ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Therapeutic Drug ◽  
Histopathological Analysis ◽  
Sw620 Cells

Abstract Recurrence and metastasis are the shortcomings of the clinical treatment of colon cancer. Finding an efficacy strategy for the treatment of colon cancer is important. In recent years, PLGA has been shown to have potential as a broad therapeutic drug delivery system. this study aimed to design a dual-loaded nanoparticles drug delivery system to overcome the limitations of chemotherapeutic drugs in colon cancer therapy. We developed epidermal growth factor (EGF) functionalized poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) co-loaded with 5-fluorouracil (5Fu) and perfluorocarbon (PFC) (EGF-PLGA@5Fu/PFC) for target therapy of colon cancer. EGF-PLGA@5Fu /PFC NPs were estimated to have an average size of 200 nm with a 5Fu-loading efficiency of 7.29%. In vitro release profile exhibited a pH-responsive release. CCK-8, Hoechst33342 staining and flow cytometry assays were performed to investigate the functions of EGF-PLGA@5Fu/PFC NPs in SW620 cells. Targeted EGF-PLGA@5Fu/PFC NPs also exhibited higher cellular uptake than non-targeted NPs in colon cancer cells. EGF-PLGA@5Fu/PFC NPs were found to have the best efficiency on cell viability suppression and apoptosis induction in SW620 cells. In xenograft mice, EGF-PLGA@5Fu/PFC NPs had the best suppressive effects on tumor growth compared with 5Fu, PLGA@5Fu and PLGA@5Fu/PFC NPs. The results of histopathological analysis further indicated that EGF-targeted NPs were the most efficient on tumor growth inhibition. Mechanically, the data demonstrated the improved therapeutic outcomes were owing to the fact that PFC could relieve tumor hypoxia via transporting oxygen to the tumor. We creatively constructed a biocompatible nanodrug delivery system and functionalized nanoparticles may provide new potential for selective delivery of chemotherapy drugs to cancers.

Recent Development of Copolymeric Nano-Drug Delivery System for Paclitaxel

2020 ◽  
Vol 20 (18) ◽  
pp. 2169-2189
Author(s):  
Shiyu Chen ◽  
Zhimei Song ◽  
Runliang Feng
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Recent Progress ◽  
Water Solubility ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Pharmacokinetic Property ◽  
Nano Drug Delivery

Background: Paclitaxel (PTX) has been clinically used for several years due to its good therapeutic effect against cancers. Its poor water-solubility, non-selectivity, high cytotoxicity to normal tissue and worse pharmacokinetic property limit its clinical application. Objective: To review the recent progress on the PTX delivery systems. Methods: In recent years, the copolymeric nano-drug delivery systems for PTX are broadly studied. It mainly includes micelles, nanoparticles, liposomes, complexes, prodrugs and hydrogels, etc. They were developed or further modified with target molecules to investigate the release behavior, targeting to tissues, pharmacokinetic property, anticancer activities and bio-safety of PTX. In the review, we will describe and discuss the recent progress on the nano-drug delivery system for PTX since 2011. Results: The water-solubility, selective delivery to cancers, tissue toxicity, controlled release and pharmacokinetic property of PTX are improved by its encapsulation into the nano-drug delivery systems. In addition, its activities against cancer are also comparable or high when compared with the commercial formulation. Conclusion: Encapsulating PTX into nano-drug carriers should be helpful to reduce its toxicity to human, keeping or enhancing its activity and improving its pharmacokinetic property.

scholarly journals Enhanced antitumor efficacy in colon cancer using EGF functionalized PLGA nanoparticles loaded with 5-Fluorouracil and perfluorocarbon

2020 ◽  
Author(s):  
pingping Wu ◽  
Qing Zhou ◽  
Huayun Zhu ◽  
Yan Zhuang ◽  
Jun Bao
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Tumor Growth ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Plga Nanoparticles ◽  
Therapeutic Drug ◽  
Histopathological Analysis ◽  
Sw620 Cells

Abstract Background: Tumor recurrence and metastasis occur at a high rate in patients with colon cancer. Identification of effective strategies for the treatment of colon cancer is critical. Recently, poly (lactic-co-glycolic acid) (PLGA) has been shown to have potential as a broad therapeutic drug delivery system. We designed a dual-loaded nanoparticle drug delivery system to overcome the limitations of chemotherapeutic drugs used to treat colon cancer. Methods: We developed epidermal growth factor (EGF) functionalized PLGA nanoparticles (NPs) co-loaded with 5-fluorouracil (5Fu) and perfluorocarbon (PFC) (EGF-PLGA@5Fu/PFC) for targeted treatment of colon cancer. CCK-8 assay, Hoechst33342 staining and flow cytometry were performed to investigate the functions of EGF-PLGA@5Fu/PFC NPs in SW620 cells. Beside, animal experiment, histological analysis and immunofluorescence staining were adopted to further confirm the role of EGF-PLGA@5Fu/PFC NPs in vivo. Results: The findings showed that EGF-PLGA@5Fu /PFC NPs had an average size 200 nm and a 5Fu-loading efficiency of 7.29%. Furthermore, in vitro release was pH-sensitive. Targeted EGF-PLGA@5Fu/PFC NPs exhibited higher cellular uptake than non-targeted NPs into colon cancer cells. In addition, EGF-PLGA@5Fu/PFC NPs suppressed cell viability and induced apoptosis in SW620 cells to a greater extent than non-targeted NPs. In tumor xenografted mice, EGF-PLGA@5Fu/PFC NPs suppressed tumor growth more effectively than 5Fu, PLGA@5Fu or PLGA@5Fu/PFC NPs. Histopathological analysis further demonstrated that EGF-targeted NPs inhibited tumor growth to a greater extent than non-targeted or non-NP treatments. The improved therapeutic outcomes observed in this study were due to relief of tumor hypoxia by transport of oxygen by PFC to the tumors. Conclusion: We constructed a biocompatible nanodrug delivery system based on functionalized nanoparticles that provided a novel strategy for selective delivery of chemotherapy drugs to tumors.

scholarly journals Novel combination for Self-nanoemulsifying Drug Delivery System of Candesartan Cilexetil

2018 ◽  
pp. 123-134
Author(s):  
Safa Fakher Mekhilef ◽  
Ahmed A. Hussein
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Solubility ◽  
Candesartan Cilexetil ◽  
Promising Result ◽  
Potential Measurement

Solubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsification time, particle size and zeta potential measurement, and in-vitro drug release. The results showed that the particle size of the best formula was 13.3 nm and zeta potential of -37.45 mV with approximately 100% release after 45 minutes .These results suggest that the preparation of CC. as SEDDS with the use of the above combination of surfactant and cosurfactant is a promising maneuver for oral delivery of CC. in order to improve its bioavailability.   

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