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Pharmaceutics, Volume 10, Issue 1

2018 March - 36 articles

Cover Story: We compared different methods, including thermodynamic models, conventional experimental screening methods, and a novel atomization screening device, in their ability to predict drug–polymer miscibility and the solid-state properties of specific drugs during the development of spray-dried amorphous solid dispersions (SDASDs). The phase behavior and solid-state properties of each sample were characterized by modulated DSC and X-ray powder diffraction. Principal component analysis was performed to assess the prediction accuracy of various screening approaches. Our novel atomization device displayed superior ability compared to conventional screening approaches in predicting the phase behavior of SDASDs, providing insights into the final properties and performance of SDASDs in early drug development.
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Articles (36)

  • Review
  • Open Access
81 Citations
59,226 Views
45 Pages

Evidence of Drug–Nutrient Interactions with Chronic Use of Commonly Prescribed Medications: An Update

  • Emily S. Mohn,
  • Hua J. Kern,
  • Edward Saltzman,
  • Susan H. Mitmesser and
  • Diane L. McKay

The long-term use of prescription and over-the-counter drugs can induce subclinical and clinically relevant micronutrient deficiencies, which may develop gradually over months or even years. Given the large number of medications currently available,...

  • Article
  • Open Access
42 Citations
9,218 Views
15 Pages

Orally Disintegrating Tablets Containing Melt Extruded Amorphous Solid Dispersion of Tacrolimus for Dissolution Enhancement

  • Poovizhi Ponnammal,
  • Parijat Kanaujia,
  • Yin Yani,
  • Wai Kiong Ng and
  • Reginald B. H. Tan

In order to improve the aqueous solubility and dissolution of Tacrolimus (TAC), amorphous solid dispersions of TAC were prepared by hot melt extrusion with three hydrophilic polymers, Polyvinylpyrrolidone vinyl acetate (PVP VA64), Soluplus® and Hydro...

(This article belongs to the Special Issue Dissolution Enhancement of Poorly Soluble Drugs)
  • Review
  • Open Access
301 Citations
18,330 Views
34 Pages

Surface-Modified Nanocarriers for Nose-to-Brain Delivery: From Bioadhesion to Targeting

  • Fabio Sonvico,
  • Adryana Clementino,
  • Francesca Buttini,
  • Gaia Colombo,
  • Silvia Pescina,
  • Silvia Stanisçuaski Guterres,
  • Adriana Raffin Pohlmann and
  • Sara Nicoli

In the field of nasal drug delivery, nose-to-brain delivery is among the most fascinating applications, directly targeting the central nervous system, bypassing the blood brain barrier. Its benefits include dose lowering and direct brain distribution...

(This article belongs to the Special Issue Nose to Brain Delivery)
  • Article
  • Open Access
123 Citations
10,876 Views
23 Pages

Lung carcinoma is the most common cancer in men and second in women (preceded by breast cancer) worldwide. Around 1 in 10 of all cancers diagnosed in men, lung cancer contributed to a total fraction of 20% cancer deaths. Naringenin (NAR) is well know...

(This article belongs to the Special Issue Nanotechnology Advances in Cancer Treatment)
  • Article
  • Open Access
16 Citations
6,253 Views
26 Pages

Biodegradable inorganic apatite-based particle complex is popular for its pH-sensitivity at the endosomal acidic environment to facilitate drug release following cellular uptake. Despite being a powerful anticancer drug, doxorubicin shows severe off-...

(This article belongs to the Special Issue Nanotechnology Advances in Cancer Treatment)
  • Article
  • Open Access
23 Citations
17,223 Views
13 Pages

Absolute Oral Bioavailability of Creatine Monohydrate in Rats: Debunking a Myth

  • Eman A. Alraddadi,
  • Ryan Lillico,
  • Jonathan L. Vennerstrom,
  • Ted M. Lakowski and
  • Donald W. Miller

Creatine is an ergogenic compound used by athletes to enhance performance. Supplementation with creatine monohydrate (CM) has been suggested for musculoskeletal and neurological disorders. Until now, little is known about its pharmacokinetic profile....

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
19 Citations
8,321 Views
26 Pages

The evaluation of drug–polymer miscibility in the early phase of drug development is essential to ensure successful amorphous solid dispersion (ASD) manufacturing. This work investigates the comparison of thermodynamic models, conventional experiment...

  • Article
  • Open Access
24 Citations
6,843 Views
21 Pages

Rational Design, Synthesis and Evaluation of γ-CD-Containing Cross-Linked Polyvinyl Alcohol Hydrogel as a Prednisone Delivery Platform

  • Adolfo Marican,
  • Fabián Avila-Salas,
  • Oscar Valdés,
  • Sergio Wehinger,
  • Jorge Villaseñor,
  • Natalia Fuentealba,
  • Mauricio Arenas-Salinas,
  • Yerko Argandoña,
  • Verónica Carrasco-Sánchez and
  • Esteban F. Durán-Lara

This study describes the in-silico rational design, synthesis and evaluation of cross-linked polyvinyl alcohol hydrogels containing γ-cyclodextrin (γ-CDHSAs) as platforms for the sustained release of prednisone (PDN). Through in-silico studies using...

  • Article
  • Open Access
35 Citations
10,313 Views
14 Pages

The evaluation of UV-filter in vitro percutaneous absorption allows the estimation of the systemic exposure dose (SED) and the margin of safety (MoS) of sunscreen products. As both the vehicle and pattern of application may affect sunscreen safety an...

  • Review
  • Open Access
428 Citations
29,682 Views
31 Pages

Ocular Drug Delivery Barriers—Role of Nanocarriers in the Treatment of Anterior Segment Ocular Diseases

  • Rinda Devi Bachu,
  • Pallabitha Chowdhury,
  • Zahraa H. F. Al-Saedi,
  • Pradeep K. Karla and
  • Sai H. S. Boddu

Ocular drug delivery is challenging due to the presence of anatomical and physiological barriers. These barriers can affect drug entry into the eye following multiple routes of administration (e.g., topical, systemic, and injectable). Topical adminis...

  • Article
  • Open Access
184 Citations
22,369 Views
22 Pages

Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrie...

(This article belongs to the Special Issue Lipid-Based Dosage Form)
  • Article
  • Open Access
3 Citations
4,956 Views
9 Pages

The objective of this work is to evaluate the potential effect of cardiac stress exercise on the accumulation of [123I]IAZA, a radiopharmaceutical used to image focal tissue hypoxia, in otherwise normal myocardium in healthy volunteers, and to determ...

  • Article
  • Open Access
25 Citations
14,346 Views
10 Pages

Epinephrine is a life-saving treatment in anaphylaxis. In community settings, a first-aid dose of epinephrine is injected from an auto-injector (EAI). Needle phobia highly contributes to EAI underuse, leading to fatalities—especially in children. A n...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
53 Citations
9,545 Views
15 Pages

Chitosan Loaded into a Hydrogel Delivery System as a Strategy to Treat Vaginal Co-Infection

  • Diego R. Perinelli,
  • Raffaella Campana,
  • Athanasios Skouras,
  • Giulia Bonacucina,
  • Marco Cespi,
  • Francesca Mastrotto,
  • Wally Baffone and
  • Luca Casettari

Polymeric hydrogels are common dosage forms designed for the topical administration of antimicrobial drugs to treat vaginal infections. One of the major advantages of using chitosan in these formulations is related to the intrinsic and broad antimicr...

(This article belongs to the Special Issue Chitosan Biomedical Applications: Opportunities and Challenges)
  • Article
  • Open Access
10 Citations
7,255 Views
16 Pages

Purpose: Hydrophobic drugs are facing a major challenge in dissolution rate enhancement and solubility in aqueous solutions; therefore, a variety of methods have been used to improve dissolution rate and/or solubility of bendroflumethiazide as a mode...

(This article belongs to the Special Issue Dissolution Enhancement of Poorly Soluble Drugs)
  • Review
  • Open Access
47 Citations
6,785 Views
12 Pages

Vascular endothelial growth factor (VEGF) plays a pivotal role in the development of neovascularization and edema from several common chorioretinal vascular conditions. The intravitreally injected drugs (aflibercept, bevacizumab, conbercept, pegaptan...

  • Article
  • Open Access
17 Citations
8,421 Views
12 Pages

Pharmacokinetics and Pharmacodynamics of (S)-Ketoprofen Co-Administered with Caffeine: A Preclinical Study in Arthritic Rats

  • Raúl Medina-López,
  • Nancy Vara-Gama,
  • Olivia Soria-Arteche,
  • Luis A. Moreno-Rocha and
  • Francisco J. López-Muñoz

The purpose of the present study was to determine whether caffeine modifies the pharmacokinetics and pharmacodynamics of (S)-ketoprofen following oral administration in a gout-type pain model. 3.2 mg/kg of (S)-ketoprofen alone and combined with 17.8...

(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
  • Review
  • Open Access
238 Citations
24,575 Views
30 Pages

Cocrystals can be used as an alternative approach based on crystal engineering to enhance specific physicochemical and biopharmaceutical properties of active pharmaceutical ingredients (APIs) when the approaches to salt or polymorph formation do not...

(This article belongs to the Special Issue Pharmaceutical Crystallisation Science and Engineering)
  • Article
  • Open Access
71 Citations
13,799 Views
12 Pages

In this work, we examined enhanced skin delivery of minoxidil applied in nanoemulsions incorporating skin penetration enhancers. Aliquots of fully characterized oil-in-water nanoemulsions (1 mL), containing minoxidil (2%) and the skin penetration enh...

  • Article
  • Open Access
36 Citations
9,016 Views
15 Pages

In this work, a novel membrane crystallization system was used to crystallize micro-sized seeds of piroxicam monohydrate by reverse antisolvent addition. Membrane crystallization seeds were compared with seeds produced by conventional antisolvent add...

(This article belongs to the Special Issue Pharmaceutical Crystallisation Science and Engineering)
  • Article
  • Open Access
10 Citations
6,939 Views
15 Pages

Meta-aminobenzoic acid, an important model system in the study of polymorphism and crystallization of active pharmaceutical ingredients, exist in water in both the nonionic (mABA) and zwitterionic (mABA±) forms. However, the constituent molecules of...

(This article belongs to the Special Issue Pharmaceutical Crystallisation Science and Engineering)
  • Review
  • Open Access
130 Citations
12,490 Views
21 Pages

A Review on Recent Advances in Stabilizing Peptides/Proteins upon Fabrication in Hydrogels from Biodegradable Polymers

  • Faisal Raza,
  • Hajra Zafar,
  • Ying Zhu,
  • Yuan Ren,
  • Aftab -Ullah,
  • Asif Ullah Khan,
  • Xinyi He,
  • Han Han,
  • Md Aquib and
  • Liang Ge
  • + 1 author

Hydrogels evolved as an outstanding carrier material for local and controlled drug delivery that tend to overcome the shortcomings of old conventional dosage forms for small drugs (NSAIDS) and large peptides and proteins. The aqueous swellable and cr...

(This article belongs to the Special Issue Protein Therapeutics)
  • Article
  • Open Access
16 Citations
9,434 Views
18 Pages

Central nervous system drug discovery and development is hindered by the impermeable nature of the blood–brain barrier. Pharmacokinetic modeling can provide a novel approach to estimate CNS drug exposure; however, existing models do not predict tempo...

(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
  • Article
  • Open Access
17 Citations
6,556 Views
8 Pages

Chitosan Gel to Treat Pressure Ulcers: A Clinical Pilot Study

  • Virginia Campani,
  • Eliana Pagnozzi,
  • Ilaria Mataro,
  • Laura Mayol,
  • Alessandra Perna,
  • Floriana D’Urso,
  • Antonietta Carillo,
  • Maria Cammarota,
  • Maria Chiara Maiuri and
  • Giuseppe De Rosa

Chitosan is biopolymer with promising properties in wound healing. Chronic wounds represent a significant burden to both the patient and the medical system. Among chronic wounds, pressure ulcers are one of the most common types of complex wound. The...

(This article belongs to the Special Issue Chitosan Biomedical Applications: Opportunities and Challenges)
  • Editorial
  • Open Access
5,004 Views
4 Pages

Canadian Pharmaceutical Scientists have a rich history of groundbreaking research in pharmacokinetics and drug metabolism undertaken primarily throughout its Pharmacy Faculties and within the Pharmaceutical and Biotechnology industry.[...]

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Review
  • Open Access
117 Citations
11,092 Views
17 Pages

Anti-microbial resistance is a growing problem that has impacted the world and brought about the beginning of the end for the old generation of antibiotics. Increasingly, more antibiotics are being prescribed unnecessarily and this reckless practice...

  • Review
  • Open Access
149 Citations
30,183 Views
31 Pages

Ophthalmic Drug Delivery Systems for Antibiotherapy—A Review

  • Marion Dubald,
  • Sandrine Bourgeois,
  • Véronique Andrieu and
  • Hatem Fessi

The last fifty years, ophthalmic drug delivery research has made much progress, challenging scientists about the advantages and limitations of this drug delivery approach. Topical eye drops are the most commonly used formulation in ocular drug delive...

  • Article
  • Open Access
12 Citations
8,454 Views
12 Pages

Is the Skin Absorption of Hydrocortisone Modified by the Variability in Dosing Topical Products?

  • Daniel A. Paterson,
  • Jacqueline Hallier,
  • Elizabeth Jenkins,
  • Sarah F. Cordery and
  • M. Begoña Delgado-Charro

Fingertip units have been proposed as a tool to standardize topical therapy with semisolid formulations. However, no studies to date have characterized the variability in dosing by patients using this concept and whether this variability ultimately a...

  • Article
  • Open Access
40 Citations
7,885 Views
16 Pages

Curcumin-Artemisinin Coamorphous Solid: Xenograft Model Preclinical Study

  • M. K. Chaitanya Mannava,
  • Kuthuru Suresh,
  • Manish Kumar Bommaka,
  • Durga Bhavani Konga and
  • Ashwini Nangia

Curcumin is a natural compound present in Indian spice turmeric. It has diverse pharmacological action but low oral solubility and bioavailability continue to limit its use as a drug. With the aim of improving the bioavailability of Curcumin (CUR), w...

(This article belongs to the Special Issue Dissolution Enhancement of Poorly Soluble Drugs)
  • Article
  • Open Access
8 Citations
5,957 Views
14 Pages

Regulation of Hepatic UGT2B15 by Methylation in Adults of Asian Descent

  • Steffen G. Oeser,
  • Jon-Paul Bingham and
  • Abby C. Collier

The hepatic uridine 5′-diphosphate-glucuronosyl transferases (UGTs) are critical for detoxifying endo- and xenobiotics. Since UGTs are also dynamically responsive to endogenous and exogenous stimuli, we examined whether epigenetic DNA methylation can...

(This article belongs to the Special Issue Pharmacokinetics and Drug Metabolism in Canada: The Current Landscape)
  • Article
  • Open Access
10 Citations
7,260 Views
18 Pages

Development of a Parenteral Formulation of NTS-Polyplex Nanoparticles for Clinical Purpose

  • María E. Aranda-Barradas,
  • Maripaz Márquez,
  • Liliana Quintanar,
  • Jaime Santoyo-Salazar,
  • Armando J. Espadas-Álvarez,
  • Daniel Martínez-Fong and
  • Elizabeth García-García

Neurotensin (NTS)-polyplex is a nanoparticle system for targeted gene delivery that holds great promise for treatment of Parkinson’s disease and various types of cancer. However, the high instability in aqueous suspension of NTS-polyplex nanoparticle...

  • Article
  • Open Access
22 Citations
6,207 Views
10 Pages

Tangeretin (TAN) is a dietary polymethoxylated flavone that possesses a broad scope of pharmacological activities. A simple high-performance liquid chromatography (HPLC) method was developed and validated in this study to quantify TAN in plasma of Sp...

(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
  • Article
  • Open Access
20 Citations
5,319 Views
11 Pages

JinQi Jiangtang (JQJT) tablets, a Chinese patent medicine approved by the State Food and Drug Administration, are composed of Coptidis Rhizoma, Astragali Radix, and Lonicerae Japonicae Flos, and have a significant effect on diabetes. Coptidis Rhizoma...

  • Review
  • Open Access
97 Citations
11,224 Views
14 Pages

GE11 Peptide as an Active Targeting Agent in Antitumor Therapy: A Minireview

  • Ida Genta,
  • Enrica Chiesa,
  • Barbara Colzani,
  • Tiziana Modena,
  • Bice Conti and
  • Rossella Dorati

A lot of solid tumors are characterized by uncontrolled signal transduction triggered by receptors related to cellular growth. The targeting of these cell receptors with antitumor drugs is essential to improve chemotherapy efficacy. This can be achie...

(This article belongs to the Special Issue Nanotechnology Advances in Cancer Treatment)
  • Feature Paper
  • Article
  • Open Access
29 Citations
15,919 Views
20 Pages

The potential of inhibitory metabolites of perpetrator drugs to contribute to drug-drug interactions (DDIs) is uncommon and underestimated. However, the occurrence of unexpected DDI suggests the potential contribution of metabolites to the observed D...

(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
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Pharmaceutics - ISSN 1999-4923