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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
68 Citations
7,507 Views
22 Pages

Development of Dual Drug Loaded Nanosized Liposomal Formulation by A Reengineered Ethanolic Injection Method and Its Pre-Clinical Pharmacokinetic Studies

  • Muhammad Sarfraz,
  • Attia Afzal,
  • Tan Yang,
  • Yongkang Gai,
  • Shahid Masood Raza,
  • Muhammad Waseem Khan,
  • Yao Cheng,
  • Xiang Ma and
  • Guangya Xiang

Oleanolic acid (OA), which is a natural pentacyclic terpenoid, has been identified for hepato-protective, nephron-protective and cardio-tonic properties. In contrast, doxorubicin (DOX) is a famous anti-cancer drug but its efficacy is a question mark...

  • Article
  • Open Access
9 Citations
6,838 Views
15 Pages

Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats

  • Tae Hwan Kim,
  • Subindra Kazi Thapa,
  • Da Young Lee,
  • Seung Eun Chung,
  • Jun Young Lim,
  • Hyeon Myeong Jeong,
  • Chang Ho Song,
  • Youn-Woong Choi,
  • Sang-Min Cho and
  • Kyu-Yeol Nam
  • + 3 authors

This study examined the effects of esomeprazole on aceclofenac pharmacokinetics and gastrointestinal complications in rats. Aceclofenac alone, or in combination with esomeprazole, was orally administered to male Sprague-Dawley rats. Plasma concentrat...

  • Article
  • Open Access
35 Citations
5,436 Views
13 Pages

We developed self-microemulsifying drug-delivery systems (SMEDDS), including bile salts, to improve the oral bioavailability of pueraria flavones (PFs). The physical properties of the SMEDDS using Cremophor RH 40, and bile salts as mixed surfactants...

  • Article
  • Open Access
148 Citations
45,499 Views
10 Pages

Franz Diffusion Cell Approach for Pre-Formulation Characterisation of Ketoprofen Semi-Solid Dosage Forms

  • Constain H. Salamanca,
  • Alvaro Barrera-Ocampo,
  • Juan C. Lasso,
  • Nathalia Camacho and
  • Cristhian J. Yarce

This study aimed to evaluate and compare, using the methodology of Franz diffusion cells, the ketoprofen (KTP) releasing profiles of two formulations: A gel and a conventional suspension. The second aim was to show that this methodology might be easi...

  • Article
  • Open Access
27 Citations
5,610 Views
14 Pages

Co-Amorphous Screening for the Solubility Enhancement of Poorly Water-Soluble Mirabegron and Investigation of Their Intermolecular Interactions and Dissolution Behaviors

  • Ji-Hun An,
  • Changjin Lim,
  • Alice Nguvoko Kiyonga,
  • In Hwa Chung,
  • In Kyu Lee,
  • Kilwoong Mo,
  • Minho Park,
  • Wonno Youn,
  • Won Rak Choi and
  • Young-Ger Suh
  • + 1 author

In the present study, the screening of Mirabegron (MBR) co-amorphous was performed to produce water-soluble and thermodynamically stable MBR co-amorphous with the purpose of overcoming the water solubility problem of MBR. MBR is Biopharmaceutics Clas...

  • Review
  • Open Access
59 Citations
6,596 Views
20 Pages

Thermo-Sensitive Vesicles in Controlled Drug Delivery for Chemotherapy

  • Elisabetta Mazzotta,
  • Lorena Tavano and
  • Rita Muzzalupo

Thermo-sensitive vesicles are a promising tool for triggering the release of drugs to solid tumours when used in combination with mild hyperthermia. Responsivity to temperature makes them intelligent nanodevices able to provide a site-specific chemot...

  • Article
  • Open Access
17 Citations
5,660 Views
16 Pages

DOX-Vit D, a Novel Doxorubicin Delivery Approach, Inhibits Human Osteosarcoma Cell Proliferation by Inducing Apoptosis While Inhibiting Akt and mTOR Signaling Pathways

  • Zaid H. Maayah,
  • Ti Zhang,
  • Marcus Laird Forrest,
  • Samaa Alrushaid,
  • Michael R. Doschak,
  • Neal M. Davies and
  • Ayman O. S. El-Kadi

Doxorubicin (DOX) is a very potent and effective anticancer agent. However, the effectiveness of DOX in osteosarcoma is usually limited by the acquired drug resistance. Recently, Vitamin D (Vit-D) was shown to suppress the growth of many human cancer...

  • Review
  • Open Access
32 Citations
6,588 Views
23 Pages

Magnetogels: Prospects and Main Challenges in Biomedical Applications

  • Sérgio R. S. Veloso,
  • Paula M. T. Ferreira,
  • J. A. Martins,
  • Paulo J. G. Coutinho and
  • Elisabete M. S. Castanheira

Drug delivery nanosystems have been thriving in recent years as a promising application in therapeutics, seeking to solve the lack of specificity of conventional chemotherapy targeting and add further features such as enhanced magnetic resonance imag...

  • Article
  • Open Access
21 Citations
5,079 Views
19 Pages

Folate and Borneol Modified Bifunctional Nanoparticles for Enhanced Oral Absorption

  • Yifan Yang,
  • Yunzhi Yin,
  • Jun Zhang,
  • Tiantian Zuo,
  • Xiao Liang,
  • Jing Li and
  • Qi Shen

Oral delivery is considered the preferred route of administration due to its convenience and favorable compliance. Here, docetaxel (DTX) loaded polylactic-co-glycolic acid (PLGA) nanoparticles, coated with polyethyleneimine–folic acid (PEI-FA) and po...

  • Article
  • Open Access
20 Citations
6,455 Views
14 Pages

Stauntonia hexaphylla leaf extract (YRA-1909), which is widely used for the antirheumatic properties, has been under phase 2 clinical trials in patients with rheumatoid arthritis since April 2017. Liquid chromatography-tandem mass spectrometric metho...

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Pharmaceutics - ISSN 1999-4923Creative Common CC BY license