Next Issue
Previous Issue

Table of Contents

Pharmaceutics, Volume 3, Issue 1 (March 2011), Pages 1-124

  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Readerexternal link to open them.
View options order results:
result details:
Displaying articles 1-7
Export citation of selected articles as:

Research

Jump to: Review

Open AccessArticle Anti-PEG IgM Response against PEGylated Liposomes in Mice and Rats
Pharmaceutics 2011, 3(1), 1-11; doi:10.3390/pharmaceutics3010001
Received: 24 November 2010 / Revised: 15 December 2010 / Accepted: 24 December 2010 / Published: 27 December 2010
Cited by 32 | PDF Full-text (173 KB) | HTML Full-text | XML Full-text
Abstract
We have reported that PEGylated liposomes lose their long-circulating properties when they are administered repeatedly at certain intervals to the same animal. This unexpected phenomenon is referred to as the accelerated blood clearance (ABC) phenomenon. We recently showed that the ABC phenomenon is
[...] Read more.
We have reported that PEGylated liposomes lose their long-circulating properties when they are administered repeatedly at certain intervals to the same animal. This unexpected phenomenon is referred to as the accelerated blood clearance (ABC) phenomenon. We recently showed that the ABC phenomenon is triggered via the abundant secretion of anti-PEG IgM in response to the first dose of PEGylated liposomes. However, the details of the underlying mechanism for the induction of anti-PEG IgM production are yet to be elucidated. The present study demonstrated that the spleen is a major organ involved in the secretion of anti-PEG IgM in mice and rats. Anti-PEG IgM production was detected in nude, T-cell deficient mice, but not in SCID mice with B- and T-cell deficiencies. These observations indicate that splenic B-cells secret anti-PEG IgM without help from T-cells. Sequential injections of PEGylated liposomes into the same mice did not promote isotype switching from IgM to IgG. Accordingly, PEGylated liposomes may function as a type-2, T-cell-independent antigen (TI-2 antigen) during anti-PEG IgM production. Although the underlying mechanism that causes an anti-PEG IgM response against PEGylated liposomes is not yet clear, our findings give implications in revealing the anti-PEG IgM response against PEGylated liposome. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
Open AccessArticle Development of a New Type of Prolonged Release Hydrocodone Formulation Based on Egalet® ADPREM Technology Using In Vivo–In Vitro Correlation
Pharmaceutics 2011, 3(1), 73-87; doi:10.3390/pharmaceutics3010073
Received: 6 February 2011 / Revised: 28 February 2011 / Accepted: 4 March 2011 / Published: 9 March 2011
Cited by 10 | PDF Full-text (444 KB) | HTML Full-text | XML Full-text
Abstract
A novel abuse deterrent, prolonged release tablet formulation of Hydrocodone for once-daily dosing has been developed, based on the novel proprietary Egalet® ADPREM technology. The tablet is an injection molded polymer system consisting of an erodible matrix in which the Active Pharmaceutical Ingredient
[...] Read more.
A novel abuse deterrent, prolonged release tablet formulation of Hydrocodone for once-daily dosing has been developed, based on the novel proprietary Egalet® ADPREM technology. The tablet is an injection molded polymer system consisting of an erodible matrix in which the Active Pharmaceutical Ingredient (API), such as Hydrocodone, is dispersed. The matrix is partly covered with a water-impermeable, non-erodible shell which leaves both ends of the cylindrical tablet exposed to erosion by the gastrointestinal (GI) fluid. In vivo–in vitro correlation (IVIVC) was initiated and validated with three formulations. A good internal predictability was observed for the three formulations. How the changing conditions in the GI tract influenced in vivo performance of an erosion based product was discussed. The validated IVIVC could be used to optimize the tablet formulation and to obtain a desired profile. In addition, this technique could help to establish the dissolution limits in which a certainty of bioequivalence is calculated. Based on this validated level A IVIVC, dissolution can be used as surrogate of bioequivalence for development, but also scale up post approval changes. Full article
(This article belongs to the Special Issue Recent Developments and Future Perspectives in Dissolution Testing)
Open AccessArticle First Quantitative Imaging of Organic Fluorine within Angiogenic Tissues by Particle Induced Gamma-Ray Emission (PIGE) Analysis: First PIGE Organic Fluorine Imaging
Pharmaceutics 2011, 3(1), 88-106; doi:10.3390/pharmaceutics3010088
Received: 31 December 2010 / Revised: 28 February 2011 / Accepted: 7 March 2011 / Published: 9 March 2011
PDF Full-text (455 KB) | HTML Full-text | XML Full-text
Abstract
PET (Positron Emission Tomography) allows imaging of the in vivo distribution of biochemical compounds labeled with a radioactive tracer, mainly 18F-FDG (2-deoxy-2-[18F] fluoro-D-glucose). 18F only allows a relatively poor spatial resolution (2-3 mm) which does not allow imaging of small tumors or specific
[...] Read more.
PET (Positron Emission Tomography) allows imaging of the in vivo distribution of biochemical compounds labeled with a radioactive tracer, mainly 18F-FDG (2-deoxy-2-[18F] fluoro-D-glucose). 18F only allows a relatively poor spatial resolution (2-3 mm) which does not allow imaging of small tumors or specific small size tissues, e.g. vasculature. Unfortunately, angiogenesis is a key process in various physiologic and pathologic processes and is, for instance, involved in modern anticancer approaches. Thus ability to visualize angiogenesis could allow early diagnosis and help to monitor the response of cancer to specific chemotherapies. Therefore, indirect analytical techniques are required to assess the localization of fluorinated compounds at a micrometric scale. Multimodality imaging approaches could provide accurate information on the metabolic activity of the target tissue. In this article, PIGE method (Particle Induced Gamma-ray Emission) was used to determine fluorinated tracers by the nuclear reaction of 19F(p,p′γ)19F in tissues. The feasibility of this approach was assessed on polyfluorinated model glucose compounds and novel peptide-based tracer designed for angiogenesis imaging. Our results describe the first mapping of the biodistribution of fluorinated compounds in both vascularized normal tissue and tumor tissue. Full article
(This article belongs to the Special Issue Molecular Imaging)
Figures

Review

Jump to: Research

Open AccessReview The Pharmacokinetics and Pharmacodynamics of Iron Preparations
Pharmaceutics 2011, 3(1), 12-33; doi:10.3390/pharmaceutics3010012
Received: 7 December 2010 / Accepted: 27 December 2010 / Published: 4 January 2011
Cited by 44 | PDF Full-text (438 KB) | HTML Full-text | XML Full-text
Abstract
Standard approaches are not appropriate when assessing pharmacokinetics of iron supplements due to the ubiquity of endogenous iron, its compartmentalized sites of action, and the complexity of the iron metabolism. The primary site of action of iron is the erythrocyte, and, in contrast
[...] Read more.
Standard approaches are not appropriate when assessing pharmacokinetics of iron supplements due to the ubiquity of endogenous iron, its compartmentalized sites of action, and the complexity of the iron metabolism. The primary site of action of iron is the erythrocyte, and, in contrast to conventional drugs, no drug-receptor interaction takes place. Notably, the process of erythropoiesis, i.e., formation of new erythrocytes, takes 3−4 weeks. Accordingly, serum iron concentration and area under the curve (AUC) are clinically irrelevant for assessing iron utilization. Iron can be administered intravenously in the form of polynuclear iron(III)-hydroxide complexes with carbohydrate ligands or orally as iron(II) (ferrous) salts or iron(III) (ferric) complexes. Several approaches have been employed to study the pharmacodynamics of iron after oral administration. Quantification of iron uptake from radiolabeled preparations by the whole body or the erythrocytes is optimal, but alternatively total iron transfer can be calculated based on known elimination rates and the intrinsic reactivity of individual preparations. Degradation kinetics, and thus the safety, of parenteral iron preparations are directly related to the molecular weight and the stability of the complex. High oral iron doses or rapid release of iron from intravenous iron preparations can saturate the iron transport system, resulting in oxidative stress with adverse clinical and subclinical consequences. Appropriate pharmacokinetics and pharmacodynamics analyses will greatly assist our understanding of the likely contribution of novel preparations to the management of anemia. Full article
Open AccessReview Nano Delivers Big: Designing Molecular Missiles for Cancer Therapeutics
Pharmaceutics 2011, 3(1), 34-52; doi:10.3390/pharmaceutics3010034
Received: 3 December 2010 / Revised: 6 January 2011 / Accepted: 11 January 2011 / Published: 13 January 2011
Cited by 22 | PDF Full-text (480 KB) | HTML Full-text | XML Full-text
Abstract
Current first-line treatments for most cancers feature a short-list of highly potent and often target-blind interventions, including chemotherapy, radiation, and surgical excision. These treatments wreak considerable havoc upon non-cancerous tissue and organs, resulting in deleterious and sometimes fatal side effects for the patient.
[...] Read more.
Current first-line treatments for most cancers feature a short-list of highly potent and often target-blind interventions, including chemotherapy, radiation, and surgical excision. These treatments wreak considerable havoc upon non-cancerous tissue and organs, resulting in deleterious and sometimes fatal side effects for the patient. In response, this past decade has witnessed the robust emergence of nanoparticles and, more relevantly, nanoparticle drug delivery systems (DDS), widely touted as the panacea of cancer therapeutics. While not a cure, nanoparticle DDS can successfully negotiate the clinical payoff between drug dosage and side effects by encompassing target-specific drug delivery strategies. The expanding library of nanoparticles includes lipoproteins, liposomes, dendrimers, polymers, metal and metal oxide nano-spheres and -rods, and carbon nanotubes, so do the modes of delivery. Importantly, however, the pharmaco-dynamics and –kinetics of these nano-complexes remain an urgent issue and a serious bottleneck in the transition from bench to bedside. This review addresses the rise of nanoparticle DDS platforms for cancer and explores concepts of gene/drug delivery and cytotoxicity in pre-clinical and clinical contexts. Full article
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
Open AccessReview Factors and Mechanisms for Pharmacokinetic Differences between Pediatric Population and Adults
Pharmaceutics 2011, 3(1), 53-72; doi:10.3390/pharmaceutics3010053
Received: 16 December 2010 / Accepted: 28 January 2011 / Published: 7 February 2011
Cited by 22 | PDF Full-text (144 KB) | HTML Full-text | XML Full-text
Abstract
Many physiologic differences between children and adults may result in age-related changes in pharmacokinetics and pharmacodynamics. Factors such as gastric pH and emptying time, intestinal transit time, immaturity of secretion and activity of bile and pancreatic fluid among other factors determine the oral
[...] Read more.
Many physiologic differences between children and adults may result in age-related changes in pharmacokinetics and pharmacodynamics. Factors such as gastric pH and emptying time, intestinal transit time, immaturity of secretion and activity of bile and pancreatic fluid among other factors determine the oral bioavailability of pediatric and adult populations. Anatomical, physiological and biochemical characteristics in children also affect the bioavailability of other routes of administration. Key factors explaining differences in drug distribution between the pediatric population and adults are membrane permeability, plasma protein binding and total body water. As far as drug metabolism is concerned, important differences have been found in the pediatric population compared with adults both for phase I and phase II metabolic enzymes. Immaturity of glomerular filtration, renal tubular secretion and tubular reabsorption at birth and their maturation determine the different excretion of drugs in the pediatric population compared to adults. Full article
Open AccessReview Cell Migration and Invasion Assays as Tools for Drug Discovery
Pharmaceutics 2011, 3(1), 107-124; doi:10.3390/pharmaceutics3010107
Received: 14 February 2011 / Revised: 3 March 2011 / Accepted: 10 March 2011 / Published: 11 March 2011
Cited by 75 | PDF Full-text (832 KB) | HTML Full-text | XML Full-text
Abstract
Cell migration and invasion are processes that offer rich targets for intervention in key physiologic and pathologic phenomena such as wound healing and cancer metastasis. With the advent of high-throughput and high content imaging systems, there has been a movement towards the use
[...] Read more.
Cell migration and invasion are processes that offer rich targets for intervention in key physiologic and pathologic phenomena such as wound healing and cancer metastasis. With the advent of high-throughput and high content imaging systems, there has been a movement towards the use of physiologically relevant cell-based assays earlier in the testing paradigm. This allows more effective identification of lead compounds and recognition of undesirable effects sooner in the drug discovery screening process. This article will review the effective use of several principle formats for studying cell motility: scratch assays, transmembrane assays, microfluidic devices and cell exclusion zone assays. Full article
(This article belongs to the Special Issue Drug Discovery Tools)

Journal Contact

MDPI AG
Pharmaceutics Editorial Office
St. Alban-Anlage 66, 4052 Basel, Switzerland
pharmaceutics@mdpi.com
Tel. +41 61 683 77 34
Fax: +41 61 302 89 18
Editorial Board
Contact Details Submit to Pharmaceutics
Back to Top