Conjugates of TAT and folate with DOX-loaded chitosan micelles offer effective intracellular delivery ability.

Abstract:

:The key for better antitumor efficacy is to improve the specificity of antitumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as antitumor drug delivery system can resolve this problem. In this study, we prepared folate and TAT (arginine-rich cell-penetrating peptide) modified N-PEG-N'-octyl-chitosan to form the folate/TAT-PEG-OC micelles. Then, the molecular structure, morphology, size distribution and bio-safety of the micelles were characterized. In order to investigate the drug-loading capacity of folate/TAT-PEG-OC micelles, doxorubicin (DOX) was used as model drug to prepare DOX-loaded chitosan micelles. Here, the confocal microscopy was used to evaluate the cellular uptake of DOX/folate/TAT-PEG-OC micelles, while the self-built NIR imaging system was used to evaluate the dynamic behavior of ICG-Der-01/folate/TAT-PEG-OC micelles in vivo. Our results demonstrate that the dual-modified PEG-OC micelles not only have good morphology, uniform size distribution and excellent drug loading capacity, but also show a strong capability for the efficient intracellular uptake and enhanced targeting behaviors in a folate receptor positive tumor model (Bel-7402 human hepatocellular cells). All these results suggest the potential application of folate/TAT-PEG-OC micelles in the targeted diagnosis and therapy to different kinds of folate receptor positive tumors.

journal_name

Pharm Dev Technol

authors

Zhang S,Liu Y,Gan Y,Qiu N,Gu Y,Zhu H

doi

10.1080/10837450.2018.1469147

subject

Has Abstract

pub_date

2019-02-01 00:00:00

pages

253-261

issue

2

eissn

1083-7450

issn

1097-9867

journal_volume

24

pub_type

杂志文章
  • Evaluation of PLGA microsphere size effect on myotoxicity using the isolated rodent skeletal muscle model.

    abstract::The present work investigated the magnitude of microsphere-induced acute myotoxicity and determined whether this myotoxicity is related to microsphere size and/or reconstitution solvent. Using a high molecular weight poly(dl-lactide-co-glycolide) copolymer, the myotoxicity of two different size microsphere formulation...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459609022596

    authors: Brazeau GA,Sciame M,al-Suwayeh SA,Fattal E

    更新日期:1996-10-01 00:00:00

  • Preparation of meloxicam-β-cyclodextrin-polyethylene glycol 6000 ternary system: characterization, in vitro and in vivo bioavailability.

    abstract::Ternary complexes of meloxicam (ML), a poorly water-soluble anti-inflammatory drug, with β-cyclodextrin (βCD) and polyethylene glycol (PEG) 6000 were prepared from an equimolar (ML-βCD) and 10% of PEG. Characterization of the ternary complex was carried out by differential scanning calorimetry and X-ray diffractometry...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.565347

    authors: Radia O,Rogalska E,Moulay-Hassane G

    更新日期:2012-09-01 00:00:00

  • Comments on prediction of the aqueous solubility using the general solubility equation (GSE) versus a genetic algorithm and a support vector machine model.

    abstract::The general solubility equation (GSE) is the state-of-the-art method for estimating the aqueous solubilities of organic compounds. It is an extremely simple equation that expresses aqueous solubility as a function of only two inputs: the octanol-water partition coefficient calculated by readily available softwares lik...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1321663

    authors: Alantary D,Yalkowsky S

    更新日期:2018-09-01 00:00:00

  • Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect.

    abstract:CONTEXT AND OBJECTIVE:The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake. MATERIALS AND METHODS:The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further opti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1055764

    authors: Banerjee S,Shankar KR,Prasad Y R

    更新日期:2016-11-01 00:00:00

  • Isolation technology for research and development applications: from concept to production.

    abstract::A prototype parenteral manufacturing facility based on isolation technology was designed, constructed, and commissioned at Warner-Lambert Co., Morris Plains, NJ, with emphasis on its application to research and development (R&D) settings. The facility contains closed isolators for holding, transferring, and manufactur...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100102034

    authors: Krishna AK,Lodhi SA,Harris MR

    更新日期:2000-01-01 00:00:00

  • Gas-saturated solution process to obtain microcomposite particles of alpha lipoic acid/hydrogenated colza oil in supercritical carbon dioxide.

    abstract::Alpha lipoic acid (ALA), an active substance in anti-aging products and dietary supplements, need to be masked with an edible polymer to obscure its unpleasant taste. However, the high viscosity of the ALA molecules prevents them from forming microcomposites with masking materials even in supercritical carbon dioxide ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1049707

    authors: Mishima K,Honjo M,Sharmin T,Ito S,Kawakami R,Kato T,Misumi M,Suetsugu T,Orii H,Kawano H,Irie K,Sano K,Mishima K,Harada T,Ouchi M

    更新日期:2016-09-01 00:00:00

  • Dry adsorbed emulsion of simvastatin: optimization and in vivo advantage.

    abstract::In the present study, Simvastatin was incorporated in emulsion of soybean oil and propylene glycol monocaprylate as oily phase and Tween 80 and Cremophor EL as surfactants and also their mixtures. Dry adsorbed emulsions were prepared by using colloidal silicon dioxide in varying proportions to adsorb the liquid emulsi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450701557246

    authors: Dixit RP,Nagarsenker MS

    更新日期:2007-01-01 00:00:00

  • Identification and characterization of potential impurities of quetiapine fumarate.

    abstract::Seven potential impurities, including by-products, starting materials and intermediates were identified in pharmaceutical substance quetiapine fumarate and characterized by spectroscopic methods (MS, IR, NMR). Based on these methods the structures of the impurities were assigned or confirmed as: impurity I: 2-(phenylt...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802409388

    authors: Stolarczyk EU,Kaczmarek L,Eksanow K,Kubiszewski M,Glice M,Kutner A

    更新日期:2009-01-01 00:00:00

  • Isotropic systems of medium-chain mono- and diglycerides for solubilization of lipophilic and hydrophilic drugs.

    abstract::The aim of this study was to investigate isotropic mono- and diglyceride-based (MCMDG) systems, which are potential vehicles for injectable products containing both hydrophilic and lipophilic drugs. For two-component systems, MCMDG was mixed with various masses of water. For three-component systems, the samples were p...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120027422

    authors: Sari P,Razzak M,Tucker IG

    更新日期:2004-01-01 00:00:00

  • Purification of pharmaceutical excipients with supercritical fluid extraction.

    abstract::Supercritical fluid extraction (SFE), with carbon dioxide as the solvent, was tested for its ability to remove common reactive impurities from several pharmaceutical excipient powders including starch, microcrystalline cellulose (MCC), hydroxypropylcellulose (HPC), polyethylene oxide (PEO), and polyvinylpyrrolidone (P...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450500299958

    authors: Ashraf-Khorassani M,Taylor LT,Waterman KC,Narayan P,Brannegan DR,Reid GL

    更新日期:2005-01-01 00:00:00

  • QbD approach to downstream processing of spray-dried amorphous solid dispersions - a case study.

    abstract::In the current study, we demonstrate a structured approach to downstream process development for spray dried amorphous solid dispersions. Direct compression is generally not suitable due to typically poor flow of spray dried powders in tablets. Roller compaction (RC) is therefore the method of choice to enable spray d...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1863985

    authors: Henriques J,Moreira J,Doktorovová S

    更新日期:2021-01-04 00:00:00

  • Polyamidoamine (PAMAM) dendrimers as potential release modulators and oral bioavailability enhancers of vardenafil hydrochloride.

    abstract::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1472611

    authors: Tawfik MA,Tadros MI,Mohamed MI

    更新日期:2019-03-01 00:00:00

  • Dynamic rheology as a quantitative method for real-time tracking of excipient solvation in non-aqueous hydroxypropylcellulose topical gels.

    abstract::This article describes a method to quantitatively track the solvation of HPC in a non-aqueous solvent system during topical gel manufacture. Where visual observation and microscopy could not establish a trend, straight-forward rheological profiling demonstrated a correlation between increased solvation of hydroxypropy...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1502319

    authors: Potuck A,Leming R,Lam S

    更新日期:2019-04-01 00:00:00

  • Novel organogels for topical delivery of naproxen: design, physicochemical characteristics and in vitro drug permeation.

    abstract::Taking into account possible irritation of the skin upon contact with naproxen (NPX) crystals and lower bioavailability after administration of the suspended or ionized drug, the aim of the work was to design and characterize novel and easy-to-formulate gels with the entirely dissolved drug in the acidic form. The for...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1135342

    authors: Osmałek T,Milanowski B,Froelich A,Górska S,Białas W,Szybowicz M,Kapela M

    更新日期:2017-06-01 00:00:00

  • Degradation of a pharmaceutical in HPLC grade methanol containing trace level formaldehyde.

    abstract::An anomalous peak was observed in the HPLC/UV analysis of a developmental drug product. High resolution LC/MS revealed that the mass of this degradant was 12 Da greater than the drug substance, corresponding to a net gain of a single carbon atom. The degradant was reproduced by incubating the drug substance with forma...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.696265

    authors: Zhong Q,Stowers S,Segraves NL,Ngim KK,Zhang K,Bostick T,Deese A,Chetwyn NP

    更新日期:2013-07-01 00:00:00

  • A new method for evaluating the dissolution of orodispersible films.

    abstract::The aim of this research was to develop and assess a new dissolution apparatus for orodispersible films (ODFs). The new apparatus was based on a flow-through cell design which requires only a limited amount of dissolution medium and can automatically collect samples in short-time intervals. Compared with the dissoluti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.882936

    authors: Xia Y,Chen F,Zhang H,Luo C

    更新日期:2015-05-01 00:00:00

  • Development of controlled-release SK&F 82526-J buffer bead formulations with tartaric acid as the buffer.

    abstract::The purpose of this research was to design and develop a novel controlled-release bead formulation for oral administration with buffer crystals as a carrier for loading of fenoldopam mesylate, an intravenous antihypertensive agent, which provides an in vitro release rate of 30-50 mg/hr for 6-8 hr. Buffer crystals were...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809028629

    authors: Venkatesh GM

    更新日期:1998-11-01 00:00:00

  • Amorphization of itraconazole by inorganic pharmaceutical excipients: comparison of excipients and processing methods.

    abstract::The aim of this study was to investigate the effects of solid carriers and processing routes on the properties of amorphous solid dispersions of itraconazole. Three solid carriers with a range of surface properties were studied, (1) a mesoporous silicate, magnesium aluminum silicate (Neusilin US2), (2) a nonporous sil...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.959181

    authors: Grobelny P,Kazakevich I,Zhang D,Bogner R

    更新日期:2015-01-01 00:00:00

  • A novel approach to increase oral drug absorption.

    abstract::A comprehensive analytical solution that accounts for many factors and assumptions affecting drug concentration profile in the gastrointestinal tract was presented. A sensitivity analysis approach was utilized in order to investigate the importance of different parameters in the model. The partition coefficient is fou...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100000741

    authors: Idkaidek NM,Abdel-Jabbar N

    更新日期:2001-01-01 00:00:00

  • Preparation and characterization of nimesulide containing nanocrystal formulations.

    abstract::The aim of this study was to develop and characterize nanocrystal formulation containing nimesulide. Physical mixture of drug and excipient (nimesulide:pluronic F127, 1:0.5) was also prepared to compare the efficiency of formulations. The physicochemical characteristics of the formulations were determined by means of ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.663390

    authors: Gülsün T,Budak C,Vural I,Sahin S,Öner L

    更新日期:2013-05-01 00:00:00

  • Influence of dissolution media pH and USP1 basket speed on erosion and disintegration characteristics of immediate release metformin hydrochloride tablets.

    abstract:PURPOSE:To investigate the influence of the pH of the dissolution medium on immediate release 850 mg metformin hydrochloride tablets. METHODS:A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP appar...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.892132

    authors: Desai D,Wong B,Huang Y,Tang D,Hemenway J,Paruchuri S,Guo H,Hsieh D,Timmins P

    更新日期:2015-01-01 00:00:00

  • Characterization of nano oxaliplatin prepared by novel Fat Employing Supercritical Nano System, the FESNS®.

    abstract:BACKGROUND:Oxaliplatin has long been used for the treatment of colorectal cancer via intra-venous infusion. In order to improve patient compliance, a solid dosage form for oral administration of oxaliplatin was prepared as nano-sized particles. METHOD:Nano oxaliplatin was prepared employing Fat Employing Supercritical...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.531735

    authors: Lee SJ,Kim YH,Lee SH,Hahn M

    更新日期:2012-03-01 00:00:00

  • In vitro/in vivo correlation and modeling of emitted dose and lung deposition of inhaled salbutamol from metered dose inhalers with different types of spacers in noninvasively ventilated patients.

    abstract::Substituting spacer by another in noninvasive ventilation (NIV) involves many variables, e.g. total emitted dose (TED), mass median aerodynamic diameter (MMAD), type of spacer, total lung deposition and total systemic absorption, which must be adjusted to ensure patient optimum therapy. Data mining based on artificial...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1116567

    authors: Hussein RRS,M A Ali A,Salem HF,Abdelrahman MM,Said ASA,Abdelrahim MEA

    更新日期:2017-11-01 00:00:00

  • Controlled-release drug delivery system based on fluocinolone acetonide-cyclodextrin inclusion complex incorporated in multivesicular liposomes.

    abstract::Multivesicular liposomes (MVLs) have been widely studied for encapsulation of hydrophilic drugs due to their structural properties and large aqueous inner cavities. In this study, to investigate MVLs and their potential application for incorporation of hydrophobic drugs, new drug delivery system for fluocinolone aceto...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.920358

    authors: Vafaei SY,Dinarvand R,Esmaeili M,Mahjub R,Toliyat T

    更新日期:2015-11-01 00:00:00

  • Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tablets.

    abstract::The objective of this study was to compare the dissolution behavior of tablets prepared from solid dispersions with and without drug-carrier interactions. Diazepam and nifedipine were used as model drugs. Two types of carriers were used; polyvinylpyrrolidone (PVP K12, K30 and K60) and saccharides (inulin 1.8 kDa, 4 kD...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903286529

    authors: Srinarong P,Kouwen S,Visser MR,Hinrichs WL,Frijlink HW

    更新日期:2010-09-01 00:00:00

  • Effect of storage conditions on the recrystallization of drugs in solid dispersions with crospovidone.

    abstract::The physical stability of amorphous solid dispersions (SDs) is influenced by their storage conditions. The goal of this work was to investigate the factors affecting the recrystallization of drugs in SDs after storage under conditions of high temperature and high humidity. SDs of three drugs (dipyridamole, nifedipine ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.795168

    authors: Shibata Y,Fujii M,Suzuki A,Koizumi N,Kanada K,Yamada M,Watanabe Y

    更新日期:2014-06-01 00:00:00

  • Reduction in burst release after coating poly(D,L-lactide-co-glycolide) (PLGA) microparticles with a drug-free PLGA layer.

    abstract::The high initial burst release of a highly water-soluble drug from poly (D,L-lactide-co-glycolide) (PLGA) microparticles prepared by the multiple emulsion (w/o/w) solvent extraction/evaporation method was reduced by coating with an additional polymeric PLGA layer. Coating with high encapsulation efficiency was perform...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.513989

    authors: Ahmed AR,Elkharraz K,Irfan M,Bodmeier R

    更新日期:2012-01-01 00:00:00

  • Design and evaluation of ocular drug delivery system for controlled delivery of gatifloxacin sesquehydrate: In vitro and in vivo evaluation.

    abstract::The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.502178

    authors: Patel UL,Chotai NP,Nagda CD

    更新日期:2012-01-01 00:00:00

  • Preparation and characterization of letrozole-loaded poly(d,l-lactide) nanoparticles for drug delivery in breast cancer therapy.

    abstract::Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism, and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to c...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1455698

    authors: Alemrayat B,Elhissi A,Younes HM

    更新日期:2019-02-01 00:00:00

  • Coprocessing of nevirapine and stavudine by spray drying.

    abstract::The objective of the present study was to coprocess 2 active pharmaceutical ingredients (APIs), nevirapine (NVP) and stavudine (STV), by spray drying technique to overcome the respective problems of poor solubility and poor content uniformity. The coprocessed product (NVP-STV CP) and untreated APIs were characterized ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802089164

    authors: Mohammed GA,Puri V,Bansal AK

    更新日期:2008-01-01 00:00:00