Water-Soluble Poly(ε-caprolactone)-Paclitaxel Prodrugs Toward an Efficient Drug Delivery System

2015 ◽  
Vol 68 (7) ◽  
pp. 1136 ◽  
Author(s):  
Ji Wang ◽  
Huanjiao Sun ◽  
Deshan Li ◽  
Jie Yuan ◽  
Xuefei Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Click Reaction ◽  
Water Soluble ◽  
Antitumour Effect ◽  
High Drug ◽  
Mercaptosuccinic Acid ◽  
Carboxylic Groups ◽  
Mtt Assays ◽  
Soluble Poly ◽  
Mcf 7

In this paper, poly(ϵ-caprolactone)-graft-carboxylic acid (P(α-C2CL)) was prepared via a thio-bromo click reaction between mercaptosuccinic acid and poly(α-bromo-ϵ-caprolactone). It is readily soluble in aqueous solutions (pH 5.5–9.8) due to the presence of carboxylic groups in each repeating unit. A series of water-soluble P(α-C2CL)-paclitaxel prodrugs with high drug contents (up to 41.4 wt-%) was prepared by esterification. Meanwhile, methyl tetrazolium (MTT) assays showed that P(α-C2CL)-paclitaxel prodrugs exhibited a high antitumour effect on A549 and MCF-7 cells. These prodrugs have appeared as a highly versatile and potent platform for cancer therapy.

Multiple strategies to produce lipophilic nanoparticles leaving water-soluble poly(HPMA)

RSC Advances ◽  
2015 ◽  
Vol 5 (83) ◽  
pp. 67475-67484 ◽  
Author(s):  
Raffaele Ferrari ◽  
Marco Callari ◽  
Davide Moscatelli
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
Produce Water ◽  
Water Soluble Polymers ◽  
Soluble Polymers ◽  
Multiple Strategies ◽  
Hydroxypropyl Methacrylamide ◽  
Drug Delivery Applications ◽  
Soluble Poly

N-(2-Hydroxypropyl) methacrylamide (HPMA) is used to produce water-soluble polymers with non-immumogenic properties that can be used in drug delivery applications.

scholarly journals Electrospun Solid Dispersions of Maraviroc for Rapid Intravaginal Preexposure Prophylaxis of HIV

2014 ◽  
Vol 58 (8) ◽  
pp. 4855-4865 ◽  
Author(s):  
Cameron Ball ◽  
Kim A. Woodrow
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Drug Loading ◽  
Solid Dispersions ◽  
High Surface ◽  
Aqueous Media ◽  
Volume Ratio ◽  
Water Soluble ◽  
High Drug ◽  
Solid Dosage

ABSTRACTThe development of topical anti-human immunodeficiency virus (HIV) microbicides may provide women with strategies to protect themselves against sexual HIV transmission. Pericoital drug delivery systems intended for use immediately before sex, such as microbicide gels, must deliver high drug doses for maximal effectiveness. The goal of achieving a high antiretroviral dose is complicated by the need to simultaneously retain the dose and quickly release drug compounds into the tissue. For drugs with limited solubility in vaginal gels, increasing the gel volume to increase the dose can result in leakage. While solid dosage forms like films and tablets increase retention, they often require more than 15 min to fully dissolve, potentially increasing the risk of inducing epithelial abrasions during sex. Here, we demonstrate that water-soluble electrospun fibers, with their high surface area-to-volume ratio and ability to disperse antiretrovirals, can serve as an alternative solid dosage form for microbicides requiring both high drug loading and rapid hydration. We formulated maraviroc at up to 28 wt% into electrospun solid dispersions made from either polyvinylpyrrolidone or poly(ethylene oxide) nanofibers or microfibers and investigated the role of drug loading, distribution, and crystallinity in determining drug release rates into aqueous media. We show here that water-soluble electrospun materials can rapidly release maraviroc upon contact with moisture and that drug delivery is faster (less than 6 min under sink conditions) when maraviroc is electrospun in polyvinylpyrrolidone fibers containing an excipient wetting agent. These materials offer an alternative dosage form to current pericoital microbicides.

Water-Soluble Poly(N-isopropylacrylamide)-Graphene Sheets Synthesized via Click Chemistry for Drug Delivery

2011 ◽  
Vol 21 (14) ◽  
pp. 2754-2763 ◽  
Author(s):  
Yongzheng Pan ◽  
Hongqian Bao ◽  
Nanda Gopal Sahoo ◽  
Tongfei Wu ◽  
Lin Li
Keyword(s):  
Drug Delivery ◽  
Click Chemistry ◽  
Water Soluble ◽  
Graphene Sheets ◽  
Soluble Poly

scholarly journals Dual-Responsive Alginate Hydrogel Constructed by Sulfhdryl Dendrimer as an Intelligent System for Drug Delivery

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 281
Author(s):  
Li Li ◽  
Dongyu Lei ◽  
Jiaojiao Zhang ◽  
Lu Xu ◽  
Jiashan Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Disulfide Bonds ◽  
Intelligent System ◽  
Click Reaction ◽  
Drug Loading ◽  
Loading Capacity ◽  
Triggered Release ◽  
High Drug ◽  
Dual Responsive ◽  
High Drug Loading

Intelligent stimulus-triggered release and high drug-loading capacity are crucial requirements for drug delivery systems in cancer treatment. Based on the excessive intracellular GSH expression and pH conditions in tumor cells, a novel glutathione (GSH) and pH dual-responsive hydrogel was designed and synthesized by conjugates of glutamic acid-cysteine dendrimer with alginate (Glu-Cys-SA) through click reaction, and then cross-linked with polyethylene glycol (PEG) through hydrogen bonds to form a 3D-net structure. The hydrogel, self-assembled by the inner disulfide bonds of the dendrimer, is designed to respond to the GSH heterogeneity in tumors, with a remarkably high drug loading capacity. The Dox-loaded Glu-Cys-SA hydrogel showed controlled drug release behavior, significantly with a release rate of over 76% in response to GSH. The cytotoxicity investigation indicated that the prepared DOX-loaded hydrogel exhibited comparable anti-tumor activity against HepG-2 cells with positive control. These biocompatible hydrogels are expected to be well-designed GSH and pH dual-sensitive conjugates or polymers for efficient anticancer drug delivery.

A copper-free click reaction for the synthesis of redox-responsive water-soluble core cross-linked nanoparticles for drug delivery in cancer therapy

2019 ◽  
Vol 21 (20) ◽  
pp. 5624-5638 ◽  
Author(s):  
Gargi Biswas ◽  
Bikash Chandra Jena ◽  
Satyagopal Sahoo ◽  
Pousali Samanta ◽  
Mahitosh Mandal ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Click Reaction ◽  
Water Soluble ◽  
Soluble Polymer ◽  
Water Soluble Polymer ◽  
Redox Responsive

Copper-free click reaction for synthesis of redox-responsive water-soluble polymer based core cross-linked nanoparticles for cancer therapy.

Design and development of high-drug-load paclitaxel (PTX)-antibody conjugates: Synthesis and preliminary evaluation of soluble paclitaxel (sPTX) and sPTX-cetuximab conjugates

2009 ◽  
Vol 27 (15_suppl) ◽  
pp. e14634-e14634
Author(s):  
A. S. Safavy ◽  
S. Quiles
Keyword(s):  
Drug Delivery ◽  
Biological Evaluation ◽  
Water Soluble ◽  
Cell Surface Receptor ◽  
Preliminary Evaluation ◽  
Breast Carcinoma Cell Line ◽  
Binding Assays ◽  
Cell Binding ◽  
Drug Load ◽  
High Drug

e14634 Background: Tumor cell surface receptor-targeted therapy of cancer is an effective treatment strategy and monoclonal antibody (MAb)-drug conjugates hold promise as tumor-specific drug delivery systems. We have previously reported the synthesis and biological evaluation of paclitaxel (PTX)-MAb conjugates using the anti-EGFR MAb, cetuximab, as an agent for tumor-targeted drug delivery system (Safavy et al., Bioconjugate Chem 14:302–310, 2003). One limitation of these conjugates was a low drug load, i.e., PTX : MAb ratios of ≤4, and thereby, low target dose delivery. Attempts to synthesize conjugates with PTX : MAb of >4 failed due to their low water solubility. As the source of this problem was identified to be the highly lipophilic PTX moiety, we hypothesized that conjugation of water-soluble PTX analogues may lead to the preservation of the MAb solubility, and thus, to the preparation of conjugates with high PTX : MAb ratios. Methods: Newly available “discrete” poly(ethylene glycol) (dPEG) linkers were utilized for the synthesis of soluble PTX analogues. In contrast to the regular PEGs wit dispersed molecular weight ranges (MWs), the dPEGs are single-MW compounds which make possible the exact dose calculation for the resulting conjugates. Solid-phase peptide synthesis methodology was used to prepare a trifunctional dPEG-lysine (K) linker, which was first conjugated to PTX to yield the water-soluble drug analogue sPTXdPEGKdPEG, containing a free carboxylic acid group. Using the latter functionality, sPTXdPEGLysdPEG was covalently conjugated to cetuximab (C225) at increasing molar ratios. Cell binding assays were performed using MCF-7 human breast carcinoma cell line. Results: sPTXC225 conjugates with PTX : C225 ratios of up to 8 were synthesized through this method, which in contrast to the previously reported conjugates, demonstrated complete aqueous solubility. Cell binding assays indicated preservation of the immunoreactivity of the parent MAb in all conjugates. Conclusions: Water-soluble and high-drug-load PTX-MAbs such as sPTXC225, may be useful for targeted delivery of therapeutically effective doses of paclitaxel and warrant further investigation. No significant financial relationships to disclose.

Formulation Optimization of Sustained Release Resinate Microcapsules of Tramadol Hydrochloride by Using 3/2 Factorial Design

2017 ◽  
Vol 6 (2) ◽  
pp. 57
Author(s):  
Kamble Ravindra K. ◽  
Chauhan Chetan S. ◽  
Kamble Priyadarshani R. ◽  
Naruka Pushpendra S.
Keyword(s):  
Drug Delivery ◽  
Ion Exchange ◽  
Sustained Release ◽  
Factorial Design ◽  
Linear Regression Analysis ◽  
Extended Period ◽  
Multiple Linear Regression Analysis ◽  
Water Soluble ◽  
Tramadol Hydrochloride ◽  
Release Drug

The main aim of the present work was to develop the microcapsules of tramadol hydrochloride for the oral sustained release drug delivery. Tramadol hydrochloride a BCS class I drug a centrally acting synthetic analgesic was complexed with Indion 254 ion exchange resin. The microcapsules were prepared by encapsulating the prepared resinates by o/o solvent evaporation technique. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of eudragit RS 100 and plasticized PEG 400. The results of multiple linear regression analysis indicated that for obtaining a sustained release drug delivery the optimum concentrations of both the plasticizer and coating solution to be used. The factorial models were used to prepare optimized microcapsules and optimized formulations showed sustained release profiles for the extended period of more than 12 hrs. From the present investigations concluded that resinate microcapsules of highly water soluble drug can provide controlled release of drug for extended period.Key Words: Tramadol hydrochloride, ion exchange resinate, microcapsules, sustained release

Development of Solid-Self Micron Emulsifying Drug Delivery Systems

2013 ◽  
Vol 6 (2) ◽  
pp. 2014-2021
Author(s):  
Preethi Sudheer ◽  
Koushik Y ◽  
Satish P ◽  
Uma Shankar M S ◽  
R S Thakur
Keyword(s):  
Drug Delivery ◽  
Systemic Circulation ◽  
Water Soluble ◽  
Future Research ◽  
Steady Increase ◽  
Liquid Form ◽  
Lipophilic Compounds ◽  
Modern Drug ◽  
Pharmaceutical Scientist ◽  
Pharmacologically Active

As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly water soluble and solubility is one of the most important parameter to achieve desired concentration of drug in systemic circulation for therapeutic response. It is a great challenge for pharmaceutical scientist to convert those molecules into orally administered formulation with sufficient bioavailability.  Among the several approaches to improve oral bioavailability of these molecules, Self-micron emulsifying drug delivery system (SMEDDS) is one of the approaches usually used to improve the bioavailability of hydrophobic drugs. However, conventional SMEDDS are mostly prepared in a liquid form, which can have several disadvantages. Accordingly, solid SMEDDS (S-SMEDDS) prepared by solidification of liquid/semisolid self-micron emulsifying (SME) ingredients into powders have gained popularity. This article provides an overview of the recent advancements in S-SMEDDS such as methodology, techniques and future research directions.

Recent Advances in Novasome Formulation Technology

2014 ◽  
Vol 7 (2) ◽  
pp. 2407-2411
Author(s):  
J M Shah ◽  
N.H Shah ◽  
Hadiya P D
Keyword(s):  
Drug Delivery ◽  
Effective Means ◽  
Entrapment Efficiency ◽  
Bilayer Membrane ◽  
Water Soluble ◽  
Delivery Methods ◽  
Liposomal Drug ◽  
Pharmaceutical Technology ◽  
Insoluble Drugs ◽  
Novel Drug

Pharmaceutical technology has developed various newer modes of novel drug delivery aspects. Modifications in the previously existing drug delivery methods have led to various newly innovated technologies serving as a safe and effective means of improvement over the existing ones. Novasome technology is one of the new innovations of liposomes which have solved many of the problems related to liposomal drug delivery system. It offers a seven bilayer membrane which has the ability to incorporate both water soluble and insoluble drugs. It has an excellent entrapment efficiency which provides better medication. Formulation of novasomes is achieved in a high shear device. Due to its numerous advantages, novasomes have been used extensively in various fields like cosmetics, chemical, personal care, foods, pharmaceuticals and agrochemicals.

Self Microemulsifying Nutraceutical and Drug Delivery Systems

2014 ◽  
Vol 7 (3) ◽  
pp. 2520-2528 ◽  
Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
The Novel ◽  
Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

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