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Pharmaceutics, Volume 9, Issue 3

2017 September - 15 articles

Cover Story: To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays, in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)-MN). The tip portions of MN completely dissolved in the rat skin within 5 min after application in vivo. After application of ALN(TIP)-MN in mice, the bioavailability of ALN was approximately 96 %. In addition, the decrease in growth plate was effectively suppressed by this efficient delivery of ALN in a rat model of osteoporosis. Furthermore, no skin irritation was observed after application of ALN(TIP)-MN. View the paper.
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Articles (15)

  • Review
  • Open Access
137 Citations
16,332 Views
27 Pages

Augmented renal clearance (ARC) is a manifestation of enhanced renal function seen in critically ill patients. The use of regular unadjusted doses of renally eliminated drugs in patients with ARC might lead to therapy failure. The purpose of this sco...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
41 Citations
8,924 Views
19 Pages

Pharmacokinetic and Toxicodynamic Characterization of a Novel Doxorubicin Derivative

  • Samaa Alrushaid,
  • Casey L. Sayre,
  • Jaime A. Yáñez,
  • M. Laird Forrest and ,
  • Sanjeewa N. Senadheera,
  • Frank J. Burczynski,
  • Raimar Löbenberg and
  • Neal M. Davies
  • + 3 authors+ 0 author

Doxorubicin (Dox) is an effective anti-cancer medication with poor oral bioavailability and systemic toxicities. DoxQ was developed by conjugating Dox to the lymphatically absorbed antioxidant quercetin to improve Dox’s bioavailability and tolerabili...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
11 Citations
6,970 Views
15 Pages

This is a comparative pharmacokinetics study of linezolid (Lzd), and two novel oxazolidinone antibacterial agents—PH027 and PH051—in rabbits to determine if the discrepancy between the in vitro and in vivo activities of the novel compounds is due to...

  • Review
  • Open Access
239 Citations
14,676 Views
11 Pages

Excised human skin is utilized for in vitro permeation experiments to evaluate the safety and effect of topically-applied drugs by measuring its skin permeation and concentration. However, ethical considerations are the major problem for using human...

(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
  • Review
  • Open Access
29 Citations
13,600 Views
16 Pages

Uridine diphosphate-glucuronosyltransferases (UGTs) are phase 2 conjugation enzymes mainly located in the endoplasmic reticulum (ER) of the liver and many other tissues, and can be recovered in artificial ER membrane preparations (microsomes). They c...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
26 Citations
17,069 Views
18 Pages

Development and Evaluation of Topical Gabapentin Formulations

  • Christopher J. Martin,
  • Natalie Alcock,
  • Sarah Hiom and
  • James C. Birchall

Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model employed, p...

  • Article
  • Open Access
11 Citations
8,555 Views
15 Pages

Pharmacokinetic Analysis of an Oral Multicomponent Joint Dietary Supplement (Phycox®) in Dogs

  • Stephanie E. Martinez,
  • Ryan Lillico,
  • Ted M. Lakowski,
  • Steven A. Martinez and
  • Neal M. Davies

Despite the lack of safety, efficacy and pharmacokinetic (PK) studies, multicomponent dietary supplements (nutraceuticals) have become increasingly popular as primary or adjunct therapies for clinical osteoarthritis in veterinary medicine. Phycox® is...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
43 Citations
8,258 Views
11 Pages

Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis

  • Hidemasa Katsumi,
  • Yutaro Tanaka,
  • Kaori Hitomi,
  • Shu Liu and ,
  • Ying-shu Quan,
  • Fumio Kamiyama,
  • Toshiyasu Sakane and
  • Akira Yamamoto
  • + 3 authors+ 0 author

To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-c...

(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
  • Article
  • Open Access
1 Citations
8,137 Views
9 Pages

While assessing the ability of mammalian lung tissue to metabolize theophylline, a new metabolite was isolated and characterized. The metabolite was produced by the microsomal fraction of lungs from several species, including rat, rabbit, dog, pig, s...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
45 Citations
12,244 Views
13 Pages

Development of Novel Faster-Dissolving Microneedle Patches for Transcutaneous Vaccine Delivery

  • Akihiko Ono,
  • Sayami Ito,
  • Shun Sakagami,
  • Hideo Asada and ,
  • Mio Saito,
  • Ying-Shu Quan,
  • Fumio Kamiyama,
  • Sachiko Hirobe and
  • Naoki Okada
  • + 4 authors+ 0 author

Microneedle (MN) patches are promising for transcutaneous vaccination because they enable vaccine antigens to physically penetrate the stratum corneum via low-invasive skin puncturing, and to be effectively delivered to antigen-presenting cells in th...

(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
  • Feature Paper
  • Article
  • Open Access
11 Citations
4,813 Views
9 Pages

A Possible Percutaneous Penetration Pathway That Should Be Considered

  • Ichiro Hatta,
  • Noboru Ohta and
  • Hiromitsu Nakazawa

The intercellular lipids in the stratum corneum form structures composed of ordered phases with orthorhombic and hexagonal hydrocarbon-chain packing structures and, in addition, a structure composed of a disordered fluid phase. Although the fluid pha...

(This article belongs to the Special Issue Recent Technology of Transdermal and Topical Drug Delivery)
  • Article
  • Open Access
7 Citations
5,634 Views
9 Pages

Veterinary Pharmaceutics: An Opportunity for Interprofessional Education in New Zealand?

  • Arlene McDowell,
  • Rebekah Beard,
  • Anna Brightmore,
  • Lisa W. Lu and ,
  • Amelia McKay,
  • Maadhuri Mistry,
  • Kate Owen,
  • Emma Swan and
  • Jessica Young
  • + 4 authors+ 0 author

Globally pharmacists are becoming increasingly involved in veterinary medicine; however, little is known about the level of interest for pharmacists playing a larger role in animal treatment in New Zealand. A key stakeholder in any progression of pha...

  • Article
  • Open Access
35 Citations
7,429 Views
13 Pages

This study was conducted to evaluate the potential benefit of particle reduction down to nanoscale on curcumin, a unique natural active compound facing therapeutic problems due to low solubility and permeability. In addition, the presence of TPGS as...

  • Article
  • Open Access
16 Citations
6,101 Views
19 Pages

Background: Fenoprofen calcium dehydrate (FCD) is counted as a non-steroidal, anti-inflammatory, anti-arthritic drug. FCD is slightly water soluble. It is indicated for mild pain relief, where the suggested dosage is 200 mg orally every 4 to 6 h. Aim...

  • Article
  • Open Access
21 Citations
7,521 Views
15 Pages

Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailability

  • Viviana De Caro,
  • Alessia Ajovalasit,
  • Flavia Maria Sutera,
  • Denise Murgia and ,
  • Maria Antonietta Sabatino and
  • Clelia Dispenza
  • + 1 author+ 0 author

Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic...

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Pharmaceutics - ISSN 1999-4923