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Pharmaceutics, Volume 10, Issue 3

September 2018 - 91 articles

Cover Story: Surfactant-based permeability enhancers are receiving increasing attention for the enhancement of the bioavailability of biopharmaceutics administered via oral or pulmonary routes. In vitro testing on intestinal Caco-2 and airway epithelial Calu-3 cells highlighted the relationship between the chemical structure of lactose-based fatty acid monoesters and their biological effects on macromolecular drug permeability. Biological studies demonstrated that the application on cells of cytotoxic concentrations above CMC was associated with depolarizing mitochondrial membrane potential, increasing nuclear membrane permeability, and activating effector caspases. Non-cytotoxic concentrations induced a reversible membrane perturbance action, as commonly exerted by surfactants acting as permeability enhancers. View this paper
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Articles (91)

  • Article
  • Open Access
9 Citations
5,601 Views
13 Pages

Characterization of CYPs and UGTs Involved in Human Liver Microsomal Metabolism of Osthenol

  • Pil Joung Cho,
  • Sanjita Paudel,
  • Doohyun Lee,
  • Yun Ji Jin,
  • GeunHyung Jo,
  • Tae Cheon Jeong,
  • Sangkyu Lee and
  • Taeho Lee

Osthenol is a prenylated coumarin isolated from the root of Angelica koreana and Angelica dahurica, and is an O-demethylated metabolite of osthole in vivo. Its various pharmacological effects have been reported previously. The metabolic pathway of os...

  • Article
  • Open Access
28 Citations
5,615 Views
13 Pages

Processing Impact on Performance of Solid Dispersions

  • Dan Zhang,
  • Yung-Chi Lee,
  • Zaher Shabani,
  • Celeste Frankenfeld Lamm,
  • Wei Zhu,
  • Yongjun Li and
  • Allen Templeton

The development of a weakly basic compound is often challenging due to changes in pH that the drug experiences throughout the gastrointestinal tract. As the drug transitions from the low pH of the stomach to the higher pH of the small intestine, drug...

  • Article
  • Open Access
19 Citations
7,768 Views
14 Pages

Development and Evaluation of a Reconstitutable Dry Suspension to Improve the Dissolution and Oral Absorption of Poorly Water-Soluble Celecoxib

  • Hye-In Kim,
  • Sang Yeob Park,
  • Seok Ju Park,
  • Jewon Lee,
  • Kwan Hyung Cho,
  • Jun-Pil Jee,
  • Hee-Cheol Kim,
  • Han-Joo Maeng and
  • Dong-Jin Jang

This study aims at developing and evaluating reconstitutable dry suspension (RDS) improved for dissolution rate, oral absorption, and convenience of use of poorly water-soluble celecoxib (CXB). Micro-sized CXB particle was used to manufacture nanosus...

  • Review
  • Open Access
190 Citations
13,646 Views
23 Pages

Lyophilization of Liposomal Formulations: Still Necessary, Still Challenging

  • Silvia Franzé,
  • Francesca Selmin,
  • Elena Samaritani,
  • Paola Minghetti and
  • Francesco Cilurzo

Nowadays, the freeze-drying of liposome dispersions is still necessary to provide a solid dosage form intended for different routes of administration (i.e., parenteral, oral, nasal and/or pulmonary). However, after decades of studies the optimization...

  • Article
  • Open Access
10 Citations
4,935 Views
14 Pages

Stabilization of the CD81 Large Extracellular Loop with De Novo Disulfide Bonds Improves Its Amenability for Peptide Grafting

  • Stefan Vogt,
  • Gerhard Stadlmayr,
  • Katharina Stadlbauer,
  • Flávio Sádio,
  • Peter Andorfer,
  • Johannes Grillari,
  • Florian Rüker and
  • Gordana Wozniak-Knopp

Tetraspan proteins are significantly enriched in the membranes of exosomal vesicles (EVs) and their extracellular domains are attractive targets for engineering towards specific antigen recognition units. To enhance the tolerance of a tetraspanin fol...

  • Article
  • Open Access
10 Citations
4,807 Views
14 Pages

Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment

  • Silvia Tampucci,
  • Daniela Monti,
  • Susi Burgalassi,
  • Eleonora Terreni,
  • Erica Zucchetti,
  • Filippo Baldacci and
  • Patrizia Chetoni

The aim of the study was the evaluation of the suitability of 5-oxo-2-pyrrolidinecarboxylic acid (PCA), also in combination with hyaluronic acid (HA), as artificial tears for treatment of dry eye syndrome (DES). Different aqueous formulations contain...

  • Feature Paper
  • Review
  • Open Access
59 Citations
6,406 Views
17 Pages

Stimuli Responsive Polymeric Systems for Cancer Therapy

  • Ali Alsuraifi,
  • Anthony Curtis,
  • Dimitrios A. Lamprou and
  • Clare Hoskins

Nanoscale polymers systems have dominated the revolution of drug delivery advancement. Their potential in the fight against cancer is unrivalled with other technologies. Their functionality increase, targeting ability and stimuli responsive nature ha...

  • Review
  • Open Access
298 Citations
15,753 Views
29 Pages

Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability

  • Maria Rosa Gigliobianco,
  • Cristina Casadidio,
  • Roberta Censi and
  • Piera Di Martino

Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of...

  • Article
  • Open Access
12 Citations
4,478 Views
14 Pages

Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

  • Ludmila A. G. Pinho,
  • Saulo G. Souza,
  • Ricardo N. Marreto,
  • Livia L. Sa-Barreto,
  • Tais Gratieri,
  • Guilherme M. Gelfuso and
  • Marcilio Cunha-Filho

The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone...

  • Article
  • Open Access
17 Citations
5,629 Views
17 Pages

DA-9805 is a botanical anti-Parkinson’s drug candidate formulated from ethanol extracts of the root of Bupleurum falcatum, the root cortex of Paeonia suffruticosa, and the root of Angelica dahurica. The pharmacokinetics (PKs) and brain distribution o...

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Pharmaceutics - ISSN 1999-4923Creative Common CC BY license