Chemotherapeutic Efficacy Enhancement in P-gp-Overexpressing Cancer Cells by Flavonoid-Loaded Polymeric Micelles.

Abstract:

:Multidrug resistance is the major problem in cancer treatment nowadays. Compounds from plants are the new targets to solve this problem. Quercetin (QCT), quercetrin (QTR), and rutin (RUT) are potential anticancer flavonoids but their poor water solubility leads to less efficacy. In this study, the polymeric micelles of benzoylated methoxy-poly (ethylene glycol)-b-oligo(ε-caprolactone) or mPEG-b-OCL-Bz loading with the flavonoids were prepared to solve these problems. The flavonoid-loaded micelles showed an average size of 13-20 nm and maximum loading capacity of 35% (w/w). The release of QCT (21%, 3 h) was lower than that of QTR (51%, 3 h) and RUT (58%, 3 h). QCT (free and micelle forms) exhibited significantly higher cytotoxicity against P-glycoprotein-overexpressing leukemia (K562/ADR) cells than QTR and RUT (p < 0.05). The results demonstrated that QCT-loaded micelles effectively reversed cytotoxicity of both doxorubicin (multidrug resistant reversing (δ) values up to 0.71) and daunorubicin (δ values up to 0.74) on K562/ADR cells. It was found that QCT-loaded micelles as well as empty polymeric micelles inhibited P-gp efflux of tetrahydropyranyl Adriamycin. Besides, mitochondrial membrane potential was decreased by QCT (in its free form and micellar formation). Our results suggested that the combination effects of polymeric micelles (inhibiting P-gp efflux) and QCT (interfering mitochondrial membrane potential) might be critical factors contributing to the reversing multidrug resistance of K562/ADR cells by QCT-loaded micelles. We concluded that QCT-loaded mPEG-b-OCL-Bz micelles are the attractive systems for overcoming multidrug-resistant cancer cells.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Khonkarn R,Daowtak K,Okonogi S

doi

10.1208/s12249-020-01657-5

subject

Has Abstract

pub_date

2020-04-26 00:00:00

pages

121

issue

4

issn

1530-9932

pii

10.1208/s12249-020-01657-5

journal_volume

21

pub_type

杂志文章
  • Product Quality Research Institute evaluation of cascade impactor profiles of pharmaceutical aerosols. Part 3. Final report on a statistical procedure for determining equivalence.

    abstract::The purpose of this article is to report final results of the evaluation of a chi-square ratio test proposed by the US Food and Drug Administration (FDA) for demonstrating equivalence of aerodynamic particle size distribution (APSD) profiles of nasal and orally inhaled drug products. A working group of the Product Qua...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0804090

    authors: Christopher D,Adams W,Amann A,Bertha C,Byron PR,Doub W,Dunbar C,Hauck W,Lyapustina S,Mitchell J,Morgan B,Nichols S,Pan Z,Singh GJ,Tougas T,Tsong Y,Wolff R,Wyka B

    更新日期:2007-11-02 00:00:00

  • Fast tablet tensile strength prediction based on non-invasive analytics.

    abstract::In this paper, linkages between tablet surface roughness, tablet compression forces, material properties, and the tensile strength of tablets were studied. Pure sodium halides (NaF, NaBr, NaCl, and NaI) were chosen as model substances because of their simple and similar structure. Based on the data available in the li...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0104-0

    authors: Halenius A,Lakio S,Antikainen O,Hatara J,Yliruusi J

    更新日期:2014-06-01 00:00:00

  • Acoustic-resonance spectrometry as a process analytical technology for the quantification of active pharmaceutical ingredient in semi-solids.

    abstract::The purpose of this study was to demonstrate acoustic resonance spectrometry (ARS) as an alternative process analytical technology to near infrared (NIR) spectroscopy for the quantification of active pharmaceutical ingredient (API) in semi-solids such as creams, gels, ointments, and lotions. The ARS used for this rese...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070359

    authors: Medendorp J,Buice RG Jr,Lodder RA

    更新日期:2006-07-14 00:00:00

  • Physicochemical and Preclinical Evaluation of a Novel Buccal Measles Vaccine.

    abstract::The aim of this study is to develop an orally disintegrating film (ODF) containing a microparticulate measles vaccine formulation for buccal delivery. The measles vaccine microparticles were made with biocompatible and biodegradable bovine serum albumin (BSA) and processed by spray drying. These vaccine microparticles...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0566-3

    authors: Gala RP,Popescu C,Knipp GT,McCain RR,Ubale RV,Addo R,Bhowmik T,Kulczar CD,D'Souza MJ

    更新日期:2017-02-01 00:00:00

  • Prodrugs of theophylline incorporating ethyleneoxy groups in the promoiety: synthesis, characterization, and transdermal delivery.

    abstract::Two different types of derivatives of theophylline (Th-H) incorporating ethyleneoxy groups into the promoiety have been synthesized. One is a soft alkyl type where N-methyl-N-methoxyethyleneoxycarbonylaminomethyl chlorides have been used to alkylate Th-H in the 7 position. The other is in an acyl type where methoxyeth...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9803-6

    authors: Majumdar S,Mueller-Spaeth M,Sloan KB

    更新日期:2012-09-01 00:00:00

  • A novel approach in distinguishing between role of hydrodynamics and mechanical stresses similar to contraction forces of GI tract on drug release from modified release dosage forms.

    abstract::The objective of this study was to determine the influence of mechanical stresses simulating gastrointestinal contraction forces of 2.0 N (stomach) and 1.2 N (intestine) on the gel properties and drug release characteristics from sustained release swelling and eroding hydrophilic matrices during dissolution studies. T...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0225-5

    authors: Takieddin M,Fassihi R

    更新日期:2015-04-01 00:00:00

  • Paul B. Myrdal, Ph.D. (June 25, 1967-May 19, 2018).

    abstract:: ...

    journal_title:AAPS PharmSciTech

    pub_type: 传,历史文章,新闻

    doi:10.1208/s12249-018-1106-0

    authors: Williams ROB 3rd

    更新日期:2018-08-01 00:00:00

  • Design and in vitro evaluation of capsaicin transdermal controlled release cubic phase gels.

    abstract::The purpose of this study was to design and investigate the transdermal controlled release cubic phase gels containing capsaicin using glycerol monooleate (MO), propylene glycol (1,2-propanediol, PG), and water. Three types of cubic phase gels were designed based on the ternary phase diagram of the MO-PG-water system,...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9481-1

    authors: Peng X,Wen X,Pan X,Wang R,Chen B,Wu C

    更新日期:2010-09-01 00:00:00

  • Essential oil formulations useful as a new tool for insect pest control.

    abstract::This study investigated the effects of some essential oils on Limantria dispar (Lepidoptera: Lymantridae, gypsy moth) larvae, one of the most serious pests of cork oak forests. The essential oils were first formulated as oil in water (o/w) emulsions and used in laboratory bioassays to assess their lethal concentration...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt030213

    authors: Moretti MD,Sanna-Passino G,Demontis S,Bazzoni E

    更新日期:2002-01-01 00:00:00

  • Characterizing and Exploring the Differences in Dissolution and Stability Between Crystalline Solid Dispersion and Amorphous Solid Dispersion.

    abstract::Solid dispersion is one of the most effective ways to improve the dissolution of insoluble drugs. When the carrier can highly disperse the drug, it will increase the wettability of the drug and reduce the surface tension, thus improving the solubility, dissolution, and bioavailability. However, amorphous solid dispers...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01802-0

    authors: Wang X,Zhang L,Ma D,Tang X,Zhang Y,Yin T,Gou J,Wang Y,He H

    更新日期:2020-09-25 00:00:00

  • Release behaviour of propranolol HCl from hydrophilic matrix tablets containing psyllium powder in combination with hydrophilic polymers.

    abstract::The objective of this study was to investigate the release behaviour of propranolol hydrochloride from psyllium matrices in the presence hydrophilic polymers. The dissolution test was carried out at pH 1.2 and pH 6.8. Binary mixtures of psyllium and hydroxypropyl methylcellulose (HPMC) used showed that an increase in ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9687-x

    authors: Siahi-Shadbad MR,Asare-Addo K,Azizian K,Hassanzadeh D,Nokhodchi A

    更新日期:2011-12-01 00:00:00

  • Excipient selection can significantly affect solid-state phase transformation in formulation during wet granulation.

    abstract::Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The influences of formulation design on the optimal dosage forms should be specified. The aim here was to investigate whether excipients with different water sorption behavior aff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt060241

    authors: Airaksinen S,Karjalainen M,Kivikero N,Westermarck S,Shevchenko A,Rantanen J,Yliruusi J

    更新日期:2005-10-06 00:00:00

  • Scale up of Semisolid Dosage Forms Manufacturing Based on Process Understanding: from Lab to Industrial Scale.

    abstract::The scale up of production processes is a major challenge in pharmaceutical industry. Using a quality by design approach, upscaling can be based on the design space, which can be assessed on a small scale. In a previous study, the critical process parameters were identified by a definitive screening design on cetomacr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1063-7

    authors: van Heugten AJP,Vromans H

    更新日期:2018-07-01 00:00:00

  • Screening of venlafaxine hydrochloride for transdermal delivery: passive diffusion and iontophoresis.

    abstract::The objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was modified to contai...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9111-3

    authors: Singh G,Ghosh B,Kaushalkumar D,Somsekhar V

    更新日期:2008-01-01 00:00:00

  • Formulation and development of extended-release micro particulate drug delivery system of solubilized rifaximin.

    abstract::Rifaximin (RFX), a semi-synthetic antibiotic belonging to BCS class IV category, has been used in the treatment of traveler's diarrhea. An attempt has been made to improve aqueous solubility of RFX in the presence of β-cyclodextrin (β-CD) and hydroxy propyl β-cyclodextrin (HP-β-CD) and control its release in the gut b...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9949-x

    authors: Karanje RV,Bhavsar YV,Jahagirdar KH,Bhise KS

    更新日期:2013-06-01 00:00:00

  • Design of lipid-based formulations for oral administration of poorly water-soluble drug fenofibrate: effects of digestion.

    abstract::Lipid-based drug carriers are likely to have influence on bioavailability through enhanced solubilization of the drug in the gastrointestinal tract. The study was designed to investigate the lipid formulation digestibility in the simulated gastro intestinal media. Fenofibrate was formulated in representative Type II, ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9787-2

    authors: Mohsin K

    更新日期:2012-06-01 00:00:00

  • Nanosuspension-Based Aloe vera Gel of Silver Sulfadiazine with Improved Wound Healing Activity.

    abstract::The present study focuses on the development and characterization of nanosuspension of a poorly soluble drug, silver sulfadiazine (SSD) incorporated in Aloe vera gel (AV-gel) for improving its therapeutic efficacy. The SSD solution in ammonia was subjected to nanoprecipitation in surfactant solution and particle size ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0817-y

    authors: Barkat MA,Harshita,Ahmad I,Ali R,Singh SP,Pottoo FH,Beg S,Ahmad FJ

    更新日期:2017-11-01 00:00:00

  • Synthesis of a semi-interpenetrating polymer network as a bioactive curcumin film.

    abstract::This study focused on the synthesis and characterization of a natural polymeric system employing the interpenetrating polymer network (IPN) comprising curcumin as a bioactive. Biopolymers and actives such as chitosan, hypromellose, citric acid, genipin, and curcumin were used to develop an effective, biodegradable, an...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0170-3

    authors: Mayet N,Kumar P,Choonara YE,Tomar LK,Tyagi C,du Toit LC,Pillay V

    更新日期:2014-12-01 00:00:00

  • Investigation of the state and dynamics of water in hydrogels of cellulose ethers by 1H NMR spectroscopy.

    abstract::The aim of this work was to study the effect of the type of substituent of the cellulose ethers and the molecular mass on the state and dynamics of water in the respective hydrogels to specify the quantity of adsorbed water on the polymers or, more explicitly, to calculate the average number of water molecules bound t...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt030436

    authors: Baumgartner S,Lahajnar G,Sepe A,Kristl J

    更新日期:2002-01-01 00:00:00

  • Ketoprofen Microemulsion for Improved Skin Delivery and In Vivo Anti-inflammatory Effect.

    abstract::We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0749-6

    authors: Aliberti ALM,de Queiroz AC,Praça FSG,Eloy JO,Bentley MVLB,Medina WSG

    更新日期:2017-10-01 00:00:00

  • PLGA Nanoparticles as Subconjunctival Injection for Management of Glaucoma.

    abstract::Nanoparticles fabricated from the biodegradable and biocompatible polymer, polylactic-co-glycolic acid (PLGA), could be a promising system for targeting ocular drug delivery. The objective of this work was to investigate the possibility of encapsulating brinzolamide in PLGA nanoparticles in order to be applied as a su...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0710-8

    authors: Salama HA,Ghorab M,Mahmoud AA,Abdel Hady M

    更新日期:2017-10-01 00:00:00

  • Effect of hydrophilic polymers on buccoadhesive Eudragit patches of propranolol hydrochloride using factorial design.

    abstract::The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive patches of propranolol hydrochloride using the hydrophobic polymer Eudragit L-100 as the base matrix. The hydrophilic polymers Carbopol 934 and polyvinyl pyrrolidone (PVP) K30 were incorporated into...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0802045

    authors: Patel VM,Prajapati BG,Patel MM

    更新日期:2007-06-22 00:00:00

  • Modeling of the Nanoparticles Absorption Under a Gastrointestinal Simulated Ambient Condition.

    abstract::Proanthocyanidins (PAs) have several bioactivities, but they are unstable in the digestive tract and possess low bioavailability. Nanoencapsulation stabilizes these compounds for oral administration. The intestinal absorption of grape seed and skin extracts, and the poly-lactic acid (PLA) nanoparticles loaded with suc...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0751-z

    authors: Fernández K,Roeckel M,Canales E,Dumont J

    更新日期:2017-10-01 00:00:00

  • Nucleic Acid-Based Therapeutics for Pulmonary Diseases.

    abstract::Nucleic acid-based therapeutics present huge potential in the treatment of pulmonary diseases ranging from lung cancer to asthma and chronic pulmonary diseases, which are often fatal and widely prevalent. The susceptibility of nucleic acids to degradation and the complex structure of lungs retard the effective pulmona...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-018-1183-0

    authors: Chen J,Tang Y,Liu Y,Dou Y

    更新日期:2018-11-01 00:00:00

  • A novel method for analyzing thick tablets by near infrared spectroscopy.

    abstract::A near-infrared (NIR) spectroscopic method to determine content uniformity of a large, thick tablet using an approach that could facilitate future validations has been developed. A CT ibuprofen 800-mg tablet weighs about 1150 mg and is about 18.6 mm wide and 7.6 mm thick. The FT NIR spectrometer was optimized for tran...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020311

    authors: Ramirez JL,Bellamy MK,Romañac RJ

    更新日期:2001-07-12 00:00:00

  • Enhanced Understanding of Pharmaceutical Materials Through Advanced Characterisation and Analysis.

    abstract::The impact of pharmaceutical materials properties on drug product quality and manufacturability is well recognised by the industry. An ongoing effort across industry and academia, the Manufacturing Classification System consortium, aims to gather the existing body of knowledge in a common framework to provide guidance...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-018-1198-6

    authors: Ferreira AP,Gamble JF,Leane MM,Park H,Olusanmi D,Tobyn M

    更新日期:2018-11-01 00:00:00

  • Simultaneous Evaluation of Dissolution and Permeation of Oral Drug Solid Formulations for Predicting Absorption Rate-Limiting Factors and In Vitro-In Vivo Correlations: Case Study Using a Poorly Soluble Weakly Basic Drug.

    abstract::Combined dissolution and permeation systems are designed to simultaneously assess the dissolution of a pharmaceutical dosage form and the permeation of dissolved drugs therefrom. However, there were still some limitations on predicting the possible absorption rate-limiting steps and improving the in vitro-in vivo corr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1544-3

    authors: Li Z,He X,Tian S,Feng G,Huang C,Xun M,Wu Z,Wang Y

    更新日期:2019-10-24 00:00:00

  • Initial characterization of micafungin pulmonary delivery via two different nebulizers and multivariate data analysis of aerosol mass distribution profiles.

    abstract::Pharmaceutical aerosols have been targeted to the lungs for the treatment of asthma and pulmonary infectious diseases successfully. Micafungin (Astellas Pharma US, Deerfield, IL, USA) has been shown to be an effective antifungal agent when administrated intravenously. Pulmonary delivery of micafungin has not previousl...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-009-9185-6

    authors: Shi S,Ashley ES,Alexander BD,Hickey AJ

    更新日期:2009-01-01 00:00:00

  • Development of Methotrexate and Minocycline Loaded Nanoparticles for the Effective Treatment of Rheumatoid Arthritis.

    abstract::Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation, and bacterial joint/bone infections. In the present work, methotrexate and minocycline-loaded nanoparticles (MMNPs) were developed with an aim to provide relief from inflammation and disease progression/join...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1581-y

    authors: Janakiraman K,Krishnaswami V,Sethuraman V,Natesan S,Rajendran V,Kandasamy R

    更新日期:2019-12-23 00:00:00

  • Mechanical Characterization and Dissolution of Chewing Gum Tablets (CGTs) Containing Co-compressed Health in Gum® and Curcumin/Cyclodextrin Inclusion Complex.

    abstract::Curcumin chewing gums could be therapeutically beneficial if used by the head and neck cancer patients. High curcumin loading in chewing gums however is needed to achieve desired therapeutic effect. Preparing gums with high drug load is nonetheless challenging because of the negative impact of solids on their masticat...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1174-1

    authors: Al Hagbani T,Altomare C,Kamal MM,Nazzal S

    更新日期:2018-11-01 00:00:00