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 such extracts was modeled, taking into consideration physicochemical process parameters, evaluating the PAs concentration profile in the human small intestine. Density (ρ), solubility, viscosity (μ), diffusion coefficient (D), and the global mass transfer coefficient (K) for both substrates were estimated, simulating their passing from the intestine into the blood at 37°C. For the seed and skin extracts encapsulated in PLA the physicochemical parameters were: D = 1.81 × 10^-5 and D = 5.72 × 10^-5 cm2/s; K = 3.4 × 10^-3 and K = 2.47 × 10^-4 cm/s, respectively. Lower resistance was offered by the seed extract than by skin extracts (nanoencapsulated), which was explained by differences in structural composition, and average molecular weight of the two kinds of extracts, which should be more favorable to the mass transfer in comparison to the raw extracts. The concentration profile of grape extracts in the small intestine was modeled through a pure convection model, and the encapsulated extract on PLA nanoparticles using a mixed regime model, which described the process of dissolution and absorption of the grape extracts from the intestine to the blood stream. The absorbed fraction predicted by the model was 42.7 and 24.2% for seed and skin extracts, respectively. Those values increased to 100% for both extracts after the simulation with the nanoencapsulated extracts. Consequently, extract encapsulation should produce a significant increase in intestinal absorption.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Fernández K,Roeckel M,Canales E,Dumont Jdoi
10.1208/s12249-017-0751-zsubject
Has Abstractpub_date
2017-10-01 00:00:00pages
2691-2701issue
7issn
1530-9932pii
10.1208/s12249-017-0751-zjournal_volume
18pub_type
杂志文章abstract：:The stability of the 37-amino acid peptide pramlintide, in aqueous solution, was studied as a function of pH and temperature. Samples of pramlintide formulated as a parenteral product were exposed to elevated temperatures and to realistic storage conditions for as long as 30 months. Pramlintide degradation was monitor...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt010207
更新日期：2000-03-18 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：:This paper reports for the first time the possible formation of a novel room temperature therapeutic deep eutectic solvent (THEDES) of risperidone (RIS) with some fatty acids, namely capric acid (C10; CA), lauric acid (C12; LA), and myristic acid (C14; MA). All mixtures of RIS and MA yielded a solid or pasty-like soli...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01844-4
更新日期：2020-11-22 00:00:00
abstract：:Low solubility of active pharmaceutical compounds (APIs) remains an important challenge in dosage form development process. In the manuscript, empirical models were developed and analyzed in order to predict dissolution of bicalutamide (BCL) from solid dispersion with various carriers. BCL was chosen as an example of ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01660-w
更新日期：2020-03-31 00:00:00
abstract：:A combination of analytical and statistical methods is used to improve a tablet coating process guided by quality by design (QbD) principles. A solid dosage form product was found to intermittently exhibit bad taste. A suspected cause was the variability in coating thickness which could lead to the subject tasting the...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-011-9723-x
更新日期：2012-03-01 00:00:00
abstract：:The objective of the present study is to investigate the confounding effects, if any, of beta-cyclodextrins (βCDs) on corneal permeability coefficients obtained from in vitro transmembrane diffusion studies. Transcorneal permeability studies were carried out with 2-hydroxypropyl-beta-cyclodextrin (HPβCD) and randomly ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0315-z
更新日期：2015-10-01 00:00:00
abstract：:High inter- and intra-individual variability in the pH of fluids in the human gastrointestinal (GI) tract has been described in the literature. The aim of this study was to assess the influence of physiological variability in fasted pH profiles of media along the GI tract on diclofenac sodium (DF-Na) dissolution from ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1140-y
更新日期：2018-10-01 00:00:00
abstract：:Cationic liposomes have long been used as non-viral vectors for small interfering RNA (siRNA) delivery but are associated with high toxicity, less transfection efficiency, and in vivo instability. In this investigation, we have developed siRNA targeted to RRM1 that is responsible for development of resistance to gemci...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0193-9
更新日期：2014-12-01 00:00:00
abstract：:The purpose of the present investigation is to formulate and evaluate proniosomal transdermal carrier systems for flurbiprofen. Proniosomes were prepared using various non-ionic surfactants, namely span 20 (Sp 20), span 40 (Sp 40), span 60 (Sp 60) and span 80 (Sp 80) without and with cholesterol at percentages ranging...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9114-0
更新日期：2008-01-01 00:00:00
abstract：:Lipid nanoparticles based on solid matrix have emerged as potential drug carriers to improve gastrointestinal (GI) absorption and oral bioavailability of several drugs, especially lipophilic compounds. These formulations may also be used for sustained drug release. Solid lipid nanoparticle (SLN) and the newer generati...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-010-9563-0
更新日期：2011-03-01 00:00:00
abstract：:Spherical granules (pellets) are quite useful in many pharmaceutical applications. The extrusion spheronisation technique is well established as a method of producing pellets of a spherical shape and narrow size distribution. After the extrusion, the cylindrical extrudates are transformed to spherical pellets by spher...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9770-y
更新日期：2012-06-01 00:00:00
abstract：:The aim of this study was to formulate a new delivery system for ecological pesticides by the incorporation of Artemisia arborescens L essential oil into solid lipid nanoparticles (SLN). Two different SLN formulations were prepared following the high-pressure homogenization technique using Compritol 888 ATO as lipid a...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070102
更新日期：2006-01-03 00:00:00
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
更新日期：2017-10-01 00:00:00
abstract：:The purpose of this research was to use inline real-time near-infrared (NIR) to measure the moisture content of granules manufactured using a commercial production scale continuous twin-screw granulator fluid-bed dryer milling process. A central composite response surface statistical design was used to study the effec...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-011-9669-z
更新日期：2011-12-01 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
abstract：:For polymer-based controlled release drug products (e.g. microspheres and implants), active pharmaceutical ingredient distribution and microporosity inside the polymer matrix are critical for product performance, particularly drug release kinetics. Due to the decreasing domain size and increasing complexity of such pr...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01741-w
更新日期：2020-07-14 00:00:00
abstract：:This investigation aimed to develop nimesulide (NMS)-loaded poly(lactic-co-glycolic acid) (PLGA)-based nanoparticulate formulations as a biodegradable polymeric drug carrier to treat rheumatoid arthritis. Polymeric nanoparticles (NPs) were prepared with two different nonionic surfactants, vitamin E d-α-tocopheryl poly...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-0048-9
更新日期：2014-02-01 00:00:00
abstract：:A melt solidification technique has been developed to obtain sustained-release waxy beads of flurbiprofen. Low glass transition temperature (t(g)) and shear-induced crystallization of flurbiprofen made it a suitable candidate for melt solidification technique. The process involved emulsification and solidification of ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040465
更新日期：2003-12-16 00:00:00
abstract：:Progesterone (PG) is a crucial immunomodulatory agent during early pregnancy, and nowadays PG oil-based injection (PG/OI) has a huge market all over the world. However, PG/OI may accumulate the local muscle and further cause irritations after long-term administration. In this study, PG nanocrystals (PG/NCs) injection ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0938-3
更新日期：2018-04-01 00:00:00
abstract：:Emulsions are widely used as topical formulations in the pharmaceutical and cosmetic industries. They are thermodynamically unstable and require emulsifiers for stabilization. Studies have indicated that emulsifiers could affect topical delivery of actives, and this study was therefore designed to investigate the effe...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0081-3
更新日期：2014-06-01 00:00:00
abstract：:This work aimed to develop a fast-dissolving film made of low dextrose equivalent maltodextrins (MDX) containing nicotine hydrogen tartrate salt (NHT). Particular attention was given to the selection of the suitable taste-masking agent (TMA) and the characterisation of the ductility and flexibility under different mec...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9525-6
更新日期：2010-12-01 00:00:00
abstract：:Direct pulmonary delivery is a promising step in developing effective gene therapies for respiratory disease. Gene therapies can be used to treat the root cause of diseases, rather than just the symptoms. However, developing effective therapies that do not cause toxicity and that successfully reach the target site at ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1215-9
更新日期：2019-01-02 00:00:00
abstract：:The purpose of this study was to prepare monodisperse gelatin microcapsules containing an active agent using microchannel (MC) emulsification, a novel technique for preparing water-in-oil (W/O) and oil-in-water (O/W) emulsions. As the first step in applying MC emulsification to the preparation of monodisperse gelatin ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt030325
更新日期：2002-01-01 00:00:00
abstract：:The purpose of this research was to investigate the measurement and in vitro delivery implications of multimodal distributions, occurring near or in the respirable range, emitted from pressurized metered-dose inhalers (pMDIs). Particle size distributions of solution pMDIs containing hydrofluoroalkane-134a (HFA-134a) a...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040338
更新日期：2003-01-01 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：:Herein, we report the successful development of a novel nanosystem capable of an efficient delivery and temperature-triggered drug release specifically aimed at cancer. The water-soluble 130.1 ± 0.2 nm iron oxide nanoparticles (IONPs) were obtained via synthesis of a monodispersed iron oxide core stabilized with tetra...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0131-x
更新日期：2014-08-01 00:00:00
abstract：:The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated as immediate release layer by using various disintegrants like Ac-D...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9116-y
更新日期：2008-01-01 00:00:00
abstract：:Onychomycosis is considered a stubborn nail fungal infection that does not respond to conventional topical antifungal treatments. This study aimed to develop and characterize novel solid lipid nanoparticles (SLNs) formulae containing terbinafine HCl (TFH) and loaded with different nail penetration enhancers (nPEs). Th...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01893-9
更新日期：2021-01-06 00:00:00
abstract：:The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle si...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0846-6
更新日期：2018-01-01 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
