Abstract：
:Triple-negative breast (TNBC) cancer that is upregulated with epidermal growth factor receptor (EGFR), and devoid of both the hormonal receptors and epidermal growth factor receptor 2 (HER 2), has led to a concept of treating TNBC with EGFR-targeted therapeutics. The combination of paclitaxel (PTX) and piperine (PIP) may improve the bioavailability of paclitaxel for cancer therapy. TPGS (vit E-PEG 1000-succinate)-coated liposomes were prepared with PTX alone or in combination with PIP, and either with (targeted) or without (non-targeted) cetuximab (CTX) conjugation. The Bradford assay indicated that 75% of CTX has been conjugated on the liposomes. The size and percent encapsulation of PTX&PIP co-loaded liposomes were found to be in the range of 204 to 218 nm and 31-73%, respectively. The drug release rate was found to be higher at pH 5.5 in comparison with release at pH 6.4 and pH 7.4. Cellular uptake and toxicity studies on MDA-MB-231 cells showed that PTX&PIP co-loaded targeted liposomes have demonstrated superior uptake and cytotoxicity than their non-targeted counterparts. The IC50 values of both of the liposomal formulations were found to be significantly higher than PTX control. Indeed, combining PIP with PTX control has improved the cytotoxicity of PTX control, which proved the synergistic anticancer effect of PIP. Lyophilized liposomes showed an excellent stability profile with the size range between 189 and 210 nm. Plasma stability study revealed a slight increase in the particle size due to the adsorption of plasma proteins on the surface of liposomes. The long-term stability study also indicated that liposomes were stable at 4°C.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Burande AS,Viswanadh MK,Jha A,Mehata AK,Shaik A,Agrawal N,Poddar S,Mahto SK,Muthu MSdoi
10.1208/s12249-020-01671-7subject
Has Abstractpub_date
2020-05-21 00:00:00pages
151issue
5issn
1530-9932pii
10.1208/s12249-020-01671-7journal_volume
21pub_type
杂志文章abstract：:Risedronate sodium (RS) is a potent inhibitor of bone resorption, having an extreme poor permeability and limited oral bioavailability (0.62%). RS should be orally administered under fasting conditions while keeping in an upright posture for at least 30 min to diminish common gastroesophageal injuries. To surmount suc...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1561-2
更新日期：2019-12-05 00:00:00
abstract：:This study was performed to prepare and characterize the biotinylated Salmon calcitonin (sCT) for oral delivery and evaluate the hypocalcemic effect of biotinylated-sCTs in rats. Biotinylated sCTs was characterized by using high performance liquid chromatography (HPLC) and MALDITOF-MS. The effect of biotinylation on p...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9165-2
更新日期：2008-01-01 00:00:00
abstract：:The approach documented in this article reviews data from earlier process validation lifecycle stages with a described statistical model to provide the "best estimate" on the number of process performance qualification (PPQ) batches that should generate sufficient information to make a scientific and risk-based decisi...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-015-0409-7
更新日期：2016-08-01 00:00:00
abstract：:Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degrad...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-0015-5
更新日期：2013-12-01 00:00:00
abstract：:Drying is one of the standard unit operations in the pharmaceutical industry and it is important to become aware of the circumstances that dominate during the process. The purpose of this study was to test microcapsulated thermochromic pigments as heat indicators in a fluid bed drying process. The indicator powders we...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-009-9351-x
更新日期：2010-03-01 00:00:00
abstract：:Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9835-y
更新日期：2012-12-01 00:00:00
abstract：:A number of synthesized chemical molecules suffer from low aqueous solubility problems. Enhancement of aqueous solubility, dissolution rate, and bioavailability of drug is a very challenging task in drug development. In the present study, solubility and dissolution of poorly aqueous soluble drug simvastatin (SIM) was ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9176-z
更新日期：2008-01-01 00:00:00
abstract：:In this study, liquid crystalline nanoparticles (LCN) have been proposed as new carrier for topical delivery of finasteride (FNS) in the treatment of androgenetic alopecia. To evaluate the potential of this nanocarrier, FNS-loaded LCN was prepared by ultrasonication method and characterized for size, shape, in vitro r...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9888-y
更新日期：2013-03-01 00:00:00
abstract：:Developing amorphous solid dispersions of water-insoluble molecules using polymeric materials is a well-defined approach to improve the dissolution rate and bioavailability. While the selected polymer plays a vital role in stabilizing the amorphous solid dispersion physically, it is equally important to improve the di...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0281-x
更新日期：2015-10-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0399-5
更新日期：2016-06-01 00:00:00
abstract：:The aim of this work was the formulation and characterization of alginate (ALG)-doxycycline (DOX) hydrogel microparticles (MPs) embedded into Pluronic F127 thermogel for DOX intradermal sustained delivery. ALG-DOX MPs were formed by adding a solution of the drug into a 1.5% polymer solution while stirring. The MPs wer...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-009-9361-8
更新日期：2010-03-01 00:00:00
abstract：:The purpose of this research was to compare the viscoelastic properties of several neutral and anionic polysaccharide polymers with their mucociliary transport rates (MTR) across explants of ciliated bovine tracheal tissue to identify rheologic parameters capable of predicting the extent of reduction in mucociliary tr...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt0802032
更新日期：2007-04-20 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0308-y
更新日期：2015-10-01 00:00:00
abstract：:Current pharmacopeial methods for in vitro orally inhaled product (OIP) performance testing were developed primarily to support requirements for drug product registration and quality control. In addition, separate clinical studies are undertaken in order to quantify safety and efficacy in the hands of the patient. How...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-016-0543-x
更新日期：2016-08-01 00:00:00
abstract：:This proof-of-concept study explores the feasibility of using a drug-loaded hydrophilic polymeric layer sandwiched between two hydrophobic layers for improving film drug load while achieving sustained release of poorly water-soluble drug. Such films having total thickness in range ~ 146-250 μm were prepared by slurry-...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1089-x
更新日期：2018-08-01 00:00:00
abstract：:The purpose of this research was to use our previously validated dynamic injection apparatus as a rapid method for screening pH-adjusted formulations of a new vancomycin analog, Van-An, for their potential to precipitate upon dilution. In 1 vial, Van-An was reconstituted according to the manufacturer's instructions. I...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070105
更新日期：2006-03-01 00:00:00
abstract：:An acid-buffering bioadhesive vaginal tablet was developed for the treatment of genitourinary tract infections. From the bioadhesion experiment and release studies it was found that polycarbophil and sodium carboxymethylcellulose is a good combination for an acid-buffering bioadhesive vaginal tablet. Sodium monocitrat...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt0804109
更新日期：2007-12-14 00:00:00
abstract：:The objective of this study was to prepare and evaluate terbutaline sulphate (TBS) bi-layer tablets for once-daily administration. The bi-layer tablets consisted of an immediate-release layer and a sustained-release layer containing 5 and 10 mg TBS, respectively. The sustained-release layer was developed by using Comp...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0404-z
更新日期：2016-06-01 00:00:00
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
更新日期：2008-01-01 00:00:00
abstract：:The classically used nontargeted chemotherapeutic approach to pancreatic cancer has a dual drawback of suboptimal drug delivery at the target site and the systemic side effects produced by the unfettered exposure of the drug to healthy tissue. This study has the objective of developing novel poly(2-ethyl-2-oxazoline) ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01745-6
更新日期：2020-08-10 00:00:00
abstract：:Ferulic acid is contained in some Chinese herbal medicines such as Ligusticum chuanxiong or Angelica sinensis. Studies have focused on the treatment of inflammatory diseases and pain using ferulic acid. However, little is known about its pharmacokinetics after transdermal administration. The present research investiga...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01709-w
更新日期：2020-06-08 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0892-0
更新日期：2018-02-01 00:00:00
abstract：:Atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs) were tested for AS sublingual permeation's feasibility as a potential alternative dosage form to treat organophosphates (OP) toxicity. More than 12,000 OP pesticide toxicity cases were reported in the USA from 2011 to 2014. AS is the recommended anti...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1420-1
更新日期：2019-06-21 00:00:00
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
更新日期：2017-02-01 00:00:00
abstract：:The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available pro...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-017-0861-7
更新日期：2018-07-01 00:00:00
abstract：:The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro poten...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070488
更新日期：2006-10-20 00:00:00
abstract：:One-third of the population of the USA suffers from metabolic syndrome (MetS). Treatment of patients with MetS regularly includes drugs prescribed simultaneously to treat diabetes and cardiovascular diseases. Therefore, the development of novel multidrug formulations is recommended. However, the main problem with thes...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1359-2
更新日期：2019-03-18 00:00:00
abstract：:The oxidation of glucagon by the H2O2/Cu(2+) system and by simulated sunlight was studied using HPLC-MS methodologies. It was found that copper ion-catalyzed oxidation is much faster in the residue 1-12 region than in photo-oxidation, but it is slower than photo-oxidation in the residue 18-29 region. This difference i...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0418-6
更新日期：2016-08-01 00:00:00
abstract：:An extract of Zingiber cassumunar Roxb. (ZC) was encapsulated in niosomes of which a topical gel was formed. (E)-4-(3',4'-dimethoxyphenyl)but-3-en-1-ol or compound D detected by a gradient HPLC was employed as the marker and its degradation determined to follow zero-order kinetics. Niosomes significantly retarded ther...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0376-z
更新日期：2016-06-01 00:00:00
abstract：:Cyclodextrins (CDs) are used in oral pharmaceutical formulations, by means of inclusion complexes formation, with the following advantages for the drugs: (1) solubility, dissolution rate, stability, and bioavailability enhancement; (2) to modify the drug release site and/or time profile; and (3) to reduce or prevent g...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-011-9690-2
更新日期：2011-12-01 00:00:00
