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Pharmaceutics, Volume 11, Issue 4

2019 April - 50 articles

Cover Story: Lignin is a natural biopolymer with well-known antioxidant capabilities. This molecule is present in the support tissues of vascular plants and provides chemical and mechanical protection from external stresses. In the present work, a method to combine LIG with poly(lactic acid) for fused filament fabrication applications is proposed. By using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, the materials were capable of reducing the concentration of this compound up to ca. 80% in 5 h. This radical scavenging activity combined with the versatility of 3D printing could be potentially beneficial for healthcare applications, especially for wound care. View this paper
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Articles (50)

  • Article
  • Open Access
22 Citations
5,882 Views
17 Pages

In order to cope with the increasing number of multimorbid patients due to demographic changes, individualized polypill solutions must be developed. One promising tool is fused layer modeling (FLM) of dosage forms with patient-specific dose combinati...

  • Article
  • Open Access
20 Citations
5,284 Views
13 Pages

Characteristics of Skin Deposition of Itraconazole Solubilized in Cream Formulation

  • Hyeongmin Kim,
  • Sukkyun Jung,
  • Sooho Yeo,
  • Dohyun Kim,
  • Young Chae Na,
  • Gyiae Yun and
  • Jaehwi Lee

Itraconazole (ITZ) is an anti-fungal agent generally used to treat cutaneous mycoses. For efficient delivery of ITZ to the skin tissues, an oil-in-water (O/W) cream formulation was developed. The O/W cream base was designed based on the solubility me...

  • Review
  • Open Access
178 Citations
26,091 Views
22 Pages

Current State and Future Perspectives on Gastroretentive Drug Delivery Systems

  • Julu Tripathi,
  • Prakash Thapa,
  • Ravi Maharjan and
  • Seong Hoon Jeong

In recent years, many attempts have been made to enhance the drug bioavailability and therapeutic effectiveness of oral dosage forms. In this context, various gastroretentive drug delivery systems (GRDDS) have been used to improve the therapeutic eff...

  • Article
  • Open Access
27 Citations
7,499 Views
12 Pages

Comparison of Salbutamol Delivery Efficiency for Jet versus Mesh Nebulizer Using Mice

  • Kyung Hwa Chang,
  • Sang-Hyub Moon,
  • Jin Young Oh,
  • Young-Soon Yoon,
  • Namyi Gu,
  • Chi-Yeon Lim,
  • Bong Joo Park and
  • Ki Chang Nam

Recent reports using a breathing simulator system have suggested that mesh nebulizers provide more effective medication delivery than jet nebulizers. In this study, the performances of jet and mesh nebulizers were evaluated by comparing their aerosol...

  • Article
  • Open Access
16 Citations
5,121 Views
16 Pages

Co-Delivery of M2e Virus-Like Particles with Influenza Split Vaccine to the Skin Using Microneedles Enhances the Efficacy of Cross Protection

  • Min-Chul Kim,
  • Ki-Hye Kim,
  • Jeong Woo Lee,
  • Yu-Na Lee,
  • Hyo-Jick Choi,
  • Yu-Jin Jung,
  • Yu-Jin Kim,
  • Richard W. Compans,
  • Mark R. Prausnitz and
  • Sang-Moo Kang

It is a high priority to develop a simple and effective delivery method for a cross-protective influenza vaccine. We investigated skin immunization by microneedle (MN) patch with human influenza split vaccine and virus-like particles containing heter...

  • Article
  • Open Access
24 Citations
5,733 Views
17 Pages

We aimed to assess the potential herb–drug interactions between Korean red ginseng extract (RGE) and metformin in rats in terms of the modulation of metformin transporters, such as organic cation transporter (Oct), multiple toxin and extrusion...

  • Article
  • Open Access
29 Citations
9,655 Views
13 Pages

Preparation and Physicochemical Stability of Liquid Oral Dosage Forms Free of Potentially Harmful Excipient Designed for Pediatric Patients

  • Guillaume Binson,
  • Karine Beuzit,
  • Virginie Migeot,
  • Léa Marco,
  • Barbara Troussier,
  • Nicolas Venisse and
  • Antoine Dupuis

Dexamethasone, hydrochlorothiazide, spironolactone, and phenytoin are commonly used in neonates, but no age-appropriate formulation containing these active pharmaceutical ingredients (APIs) is commercially available. Thus, pharmaceutical compounding...

  • Article
  • Open Access
37 Citations
5,517 Views
15 Pages

The multiple causes of cardiovascular diseases signify a major incidence and developmental risk of this pathology. One of the processes accountable for this pathologic development is the instauration of dysbiosis and its connection with an inflammato...

  • Article
  • Open Access
45 Citations
5,196 Views
22 Pages

Gellan Gum/Laponite Beads for the Modified Release of Drugs: Experimental and Modeling Study of Gastrointestinal Release

  • Alessandra Adrover,
  • Patrizia Paolicelli,
  • Stefania Petralito,
  • Laura Di Muzio,
  • Jordan Trilli,
  • Stefania Cesa,
  • Ingunn Tho and
  • Maria Antonietta Casadei

In this study, gellan gum (GG), a natural polysaccharide, was used to fabricate spherical porous beads suitable as sustained drug delivery systems for oral administration. GG was cross-linked with calcium ions to prepare polymeric beads. Rheological...

  • Article
  • Open Access
94 Citations
8,350 Views
21 Pages

Long-acting topical products for pre-exposure prophylaxis (PrEP) that combine antiretrovirals (ARVs) inhibiting initial stages of infection are highly promising for prevention of HIV sexual transmission. We fabricated core-shell poly(lactide-co-glyco...

  • Article
  • Open Access
43 Citations
5,632 Views
16 Pages

Phytosterols are plant sterols recommended as adjuvant therapy for hypercholesterolemia and tocopherols are well-established anti-oxidants. However, thermo-sensitivity, lipophilicity and formulation-dependent efficacy bring challenges in the developm...

  • Article
  • Open Access
19 Citations
6,196 Views
16 Pages

Phospholipid-Based Prodrugs for Colon-Targeted Drug Delivery: Experimental Study and In-Silico Simulations

  • Milica Markovic,
  • Arik Dahan,
  • Shahar Keinan,
  • Igor Kurnikov,
  • Aaron Aponick,
  • Ellen M. Zimmermann and
  • Shimon Ben-Shabat

In ulcerative colitis (UC), the inflammation is localized in the colon, and one of the successful strategies for colon-targeting drug delivery is the prodrug approach. In this work, we present a novel phospholipid (PL)-based prodrug approach, as a to...

  • Article
  • Open Access
34 Citations
6,617 Views
22 Pages

In this study, we examined the effect of cationic lipid type in folate (FA)-polyethylene glycol (PEG)-modified cationic liposomes on gene-silencing effects in tumor cells using cationic liposomes/siRNA complexes (siRNA lipoplexes). We used three type...

  • Review
  • Open Access
196 Citations
12,617 Views
17 Pages

Electrospun Nanofibers for Tissue Engineering with Drug Loading and Release

  • Kaiqiang Ye,
  • Haizhu Kuang,
  • Zhengwei You,
  • Yosry Morsi and
  • Xiumei Mo

Electrospinning technologies have been applied in the field of tissue engineering as materials, with nanoscale-structures and high porosity, can be easily prepared via this method to bio-mimic the natural extracellular matrix (ECM). Tissue engineerin...

  • Article
  • Open Access
8 Citations
4,782 Views
14 Pages

Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, a...

  • Article
  • Open Access
59 Citations
8,340 Views
19 Pages

In Vivo Biocompatibility of Electrospun Biodegradable Dual Carrier (Antibiotic + Growth Factor) in a Mouse Model—Implications for Rapid Wound Healing

  • Charu Dwivedi,
  • Himanshu Pandey,
  • Avinash C. Pandey,
  • Sandip Patil,
  • Pramod W. Ramteke,
  • Peter Laux,
  • Andreas Luch and
  • Ajay Vikram Singh

Tissue engineering technologies involving growth factors have produced one of the most advanced generations of diabetic wound healing solutions. Using this approach, a nanocomposite carrier was designed using Poly(d,l-lactide-co-glycolide) (PLGA)/Gel...

  • Article
  • Open Access
46 Citations
8,915 Views
17 Pages

Biodistribution and Physiologically-Based Pharmacokinetic Modeling of Gold Nanoparticles in Mice with Interspecies Extrapolation

  • Mohamed Aborig,
  • Paul R. V. Malik,
  • Shruti Nambiar,
  • Pierre Chelle,
  • Johnson Darko,
  • Anthony Mutsaers,
  • Andrea N. Edginton,
  • Andre Fleck,
  • Ernest Osei and
  • Shawn Wettig

Gold nanoparticles (AuNPs) are a focus of growing medical research applications due to their unique chemical, electrical and optical properties. Because of uncertain toxicity, “green” synthesis methods are emerging, using plant extracts t...

  • Article
  • Open Access
83 Citations
7,095 Views
13 Pages

Dual pH/Redox-Responsive Mixed Polymeric Micelles for Anticancer Drug Delivery and Controlled Release

  • Yongle Luo,
  • Xujun Yin,
  • Xi Yin,
  • Anqi Chen,
  • Lili Zhao,
  • Gang Zhang,
  • Wenbo Liao,
  • Xiangxuan Huang,
  • Juan Li and
  • Can Yang Zhang

Stimuli-responsive polymeric micelles (PMs) have shown great potential in drug delivery and controlled release in cancer chemotherapy. Herein, inspired by the features of the tumor microenvironment, we developed dual pH/redox-responsive mixed PMs whi...

  • Article
  • Open Access
2 Citations
4,156 Views
11 Pages

Cell Internalization in Fluidic Culture Conditions Is Improved When Microparticles Are Specifically Targeted to the Human Epidermal Growth Factor Receptor 2 (HER2)

  • Inmaculada Mora-Espí,
  • Elena Ibáñez,
  • Jorge Soriano,
  • Carme Nogués,
  • Thorarinn Gudjonsson and
  • Leonardo Barrios

Purpose: To determine if the specific targeting of microparticles improves their internalization by cells under fluidic conditions. Methods: Two isogenic breast epithelial cell lines, one overexpressing the Human Epidermal Growth Factor Receptor 2 (H...

  • Article
  • Open Access
22 Citations
4,371 Views
20 Pages

Background: Associating paclitaxel (PTX) to doxorubicin (DXR) is one of the main chemotherapy strategies for breast cancer (BC) management. Protocols currently available consist in administering both drugs on their maximum tolerated dose, not taking...

  • Article
  • Open Access
6 Citations
4,099 Views
17 Pages

Solid dispersions are important supersaturating formulations to orally deliver poorly water-soluble drugs. A most important process technique is hot melt extrusion but process requirements limit the choice of suitable polymers. One way around this li...

  • Article
  • Open Access
15 Citations
4,557 Views
24 Pages

Two size classes of piroxicam (PXC) pellets (mini (380–550 μm) and conventional (700–1200 μm)) were prepared using extrusion/spheronization and medium viscosity chitosan (CHS). Mixture experimental design and numerical optimization...

  • Meeting Report
  • Open Access
11 Citations
4,166 Views
11 Pages

Age-Related Medicine

  • John Wahlich,
  • Mine Orlu,
  • Alpana Mair,
  • Sven Stegemann and
  • Diana van Riet-Nales

A meeting organised by the Academy of Pharmaceutical Sciences focussed on the challenges of developing medicines for older adults. International experts discussed the complexity introduced by polypharmacy and multiple morbidities and how the risk&nda...

  • Article
  • Open Access
51 Citations
8,280 Views
29 Pages

Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV

  • Ashana Puri,
  • Sonalika A. Bhattaccharjee,
  • Wei Zhang,
  • Meredith Clark,
  • Onkar N. Singh,
  • Gustavo F. Doncel and
  • Ajay K. Banga

Tenofovir alafenamide (TAF) is an effective nucleotide reverse transcriptase inhibitor that is used in the treatment of HIV-1 and HBV. Currently, it is being investigated for HIV prophylaxis. Oral TAF regimens require daily intake, which hampers adhe...

  • Article
  • Open Access
4 Citations
4,527 Views
14 Pages

Peripheral arterial disease (PAD) is often characterized by continued reduction in blood flow supply to limbs. Advanced therapeutic strategies like gene therapy could potentially be applied to limb ischemia therapy. However, developing a gene deliver...

  • Article
  • Open Access
9 Citations
4,471 Views
16 Pages

Mechanistic Studies on the Absorption-Enhancing Effects of Gemini Surfactant on the Intestinal Absorption of Poorly Absorbed Hydrophilic Drugs in Rats

  • Tammam Alama,
  • Kosuke Kusamori,
  • Masaki Morishita,
  • Hidemasa Katsumi,
  • Toshiyasu Sakane and
  • Akira Yamamoto

Generally, the use of absorption enhancers might be the most effective approaches to ameliorate the enteric absorption of poorly absorbed substances. Among numerous absorption enhancers, we already reported that a gemini surfactant, sodium dilauramid...

  • Article
  • Open Access
29 Citations
4,352 Views
12 Pages

Cytotoxic Effect of Paclitaxel and Lapatinib Co-Delivered in Polylactide-co-Poly(ethylene glycol) Micelles on HER-2-Negative Breast Cancer Cells

  • Alicja Zajdel,
  • Adam Wilczok,
  • Katarzyna Jelonek,
  • Monika Musiał-Kulik,
  • Aleksander Foryś,
  • Suming Li and
  • Janusz Kasperczyk

To find better strategies to enhance the cytotoxic effect of paclitaxel (PTX) and lapatinib (LAP) against breast cancer cells, we analyzed the efficacy of a novel delivery system containing polylactide-co-poly(ethylene glycol) (PLA-PEG) filomicelles...

  • Review
  • Open Access
61 Citations
13,654 Views
32 Pages

Extrapolation of pharmacokinetic (PK) parameters from in vitro or in vivo animal to human is one of the main tasks in the drug development process. Translational approaches provide evidence for go or no-go decision-making during drug discovery and th...

  • Article
  • Open Access
5 Citations
3,963 Views
14 Pages

The use of lipid-based formulations (LBFs) in improving the absorption of poorly water-soluble drugs has now well established. Because the in vivo evaluation of LBFs is labor-intensive, in vitro or ex vivo approaches could provide advantages. In this...

  • Article
  • Open Access
251 Citations
17,393 Views
14 Pages

Antioxidant PLA Composites Containing Lignin for 3D Printing Applications: A Potential Material for Healthcare Applications

  • Juan Domínguez-Robles,
  • Niamh K. Martin,
  • Mun Leon Fong,
  • Sarah A. Stewart,
  • Nicola J. Irwin,
  • María Isabel Rial-Hermida,
  • Ryan F. Donnelly and
  • Eneko Larrañeta

Lignin (LIG) is a natural biopolymer with well-known antioxidant capabilities. Accordingly, in the present work, a method to combine LIG with poly(lactic acid) (PLA) for fused filament fabrication applications (FFF) is proposed. For this purpose, PLA...

  • Review
  • Open Access
105 Citations
8,567 Views
17 Pages

A New Hope: Self-Assembling Peptides with Antimicrobial Activity

  • Lucia Lombardi,
  • Annarita Falanga,
  • Valentina Del Genio and
  • Stefania Galdiero

Peptide drugs hold great promise for the treatment of infectious diseases thanks to their novel mechanisms of action, low toxicity, high specificity, and ease of synthesis and modification. Naturally developing self-assembly in nature has inspired re...

  • Article
  • Open Access
19 Citations
5,234 Views
16 Pages

Tuning the Transdermal Delivery of Hydroquinone upon Formulation with Novel Permeation Enhancers

  • Dolores R. Serrano,
  • María José Gordo,
  • Antonio Matji,
  • Salvador González,
  • Aikaterini Lalatsa and
  • Juan José Torrado

Hydroquinone (HQ) is an anti-hyperpigmentation agent with poor physicochemical stability. HQ formulations are currently elaborated by compounding in local pharmacies. Variability in the characteristics of HQ topical formulations can lead to remarkabl...

  • Article
  • Open Access
12 Citations
6,324 Views
13 Pages

A continuous-spray granulator (CTS-SGR) is a one-step granulation technology capable of using solutions or suspensions. The present research objectives were, (1) to reduce the manufacturing operations for solid dosage formulations, (2) to make amorph...

  • Review
  • Open Access
13 Citations
3,981 Views
31 Pages

Relating Advanced Electrospun Fiber Architectures to the Temporal Release of Active Agents to Meet the Needs of Next-Generation Intravaginal Delivery Applications

  • Kevin M. Tyo,
  • Farnaz Minooei,
  • Keegan C. Curry,
  • Sarah M. NeCamp,
  • Danielle L. Graves,
  • Joel R. Fried and
  • Jill M. Steinbach-Rankins

Electrospun fibers have emerged as a relatively new delivery platform to improve active agent retention and delivery for intravaginal applications. While uniaxial fibers have been explored in a variety of applications including intravaginal delivery,...

  • Article
  • Open Access
49 Citations
5,082 Views
14 Pages

Release Profile of Gentamicin Sulfate from Polylactide-co-Polycaprolactone Electrospun Nanofiber Matrices

  • Silvia Pisani,
  • Rossella Dorati,
  • Enrica Chiesa,
  • Ida Genta,
  • Tiziana Modena,
  • Giovanna Bruni,
  • Pietro Grisoli and
  • Bice Conti

The advent and growth of resistance phenomena to antibiotics has reached critical levels, invalidating the action of a majority of antibiotic drugs currently used in the clinical field. Several innovative techniques, such as the nanotechnology, can b...

  • Article
  • Open Access
15 Citations
5,208 Views
13 Pages

Pharmacokinetics and Metabolism of Acetyl Triethyl Citrate, a Water-Soluble Plasticizer for Pharmaceutical Polymers in Rats

  • Hyeon Kim,
  • Young Seok Ji,
  • Shaheed Ur Rehman,
  • Min Sun Choi,
  • Myung Chan Gye and
  • Hye Hyun Yoo

Acetyl triethyl citrate (ATEC) is a water-soluble plasticizer used in pharmaceutical plasticized polymers. In this study, the pharmacokinetics and metabolism of ATEC were investigated using liquid chromatography–tandem mass spectrometry (LC&nda...

  • Article
  • Open Access
55 Citations
5,668 Views
35 Pages

Co-Delivery of Eugenol and Dacarbazine by Hyaluronic Acid-Coated Liposomes for Targeted Inhibition of Survivin in Treatment of Resistant Metastatic Melanoma

  • Harshita Mishra,
  • Pawan Kumar Mishra,
  • Zeenat Iqbal,
  • Manu Jaggi,
  • Alka Madaan,
  • Kimi Bhuyan,
  • Namita Gupta,
  • Neha Gupta,
  • Karnika Vats and
  • Sushama Talegaonkar
  • + 1 author

While melanoma remains a challenge for oncologists, possibilities are being continuously explored to fight resistant metastatic melanoma more effectively. Eugenol is reported to inhibit survivin protein in breast cancer cells. Survivin is also overex...

  • Article
  • Open Access
42 Citations
4,948 Views
18 Pages

Phyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessib...

  • Article
  • Open Access
11 Citations
3,005 Views
10 Pages

Ultrasound assisted compression (USAC) is a manufacturing technique which applies thermal and mechanical energy to the powder bed, producing tablets with improved characteristics compared to the direct compression process. This technology is ideal fo...

  • Article
  • Open Access
14 Citations
4,536 Views
14 Pages

Melt-Cast Films Significantly Enhance Triamcinolone Acetonide Delivery to the Deeper Ocular Tissues

  • Akshaya Tatke,
  • Narendar Dudhipala,
  • Karthik Yadav Janga,
  • Bhavik Soneta,
  • Bharathi Avula and
  • Soumyajit Majumdar

Delivering an effective drug load to the posterior section of the ocular tissues, while using a non-invasive technique, has always been a challenge. In this regard, the goal of the present study was to develop sustained release triamcinolone acetonid...

  • Article
  • Open Access
38 Citations
5,400 Views
12 Pages

Feasibility Study of Mesoporous Silica Particles for Pulmonary Drug Delivery: Therapeutic Treatment with Dexamethasone in a Mouse Model of Airway Inflammation

  • Tina Gulin-Sarfraz,
  • Sofia Jonasson,
  • Elisabeth Wigenstam,
  • Eva von Haartman,
  • Anders Bucht and
  • Jessica M. Rosenholm

Diseases in the respiratory tract rank among the leading causes of death in the world, and thus novel and optimized treatments are needed. The lungs offer a large surface for drug absorption, and the inhalation of aerosolized drugs are a well-establi...

  • Communication
  • Open Access
84 Citations
8,317 Views
10 Pages

Drop-On-Powder 3D Printing of Tablets with an Anti-Cancer Drug, 5-Fluorouracil

  • Kejing Shi,
  • Deck K. Tan,
  • Ali Nokhodchi and
  • Mohammed Maniruzzaman

This study reports the first case of an innovative drop-on-powder (DoP) three-dimensional (3D) printing technology to produce oral tablets (diameters of 10 mm and 13 mm) loaded with an anticancer model drug, 5-fluorouracil (FLU). For this study, a co...

  • Article
  • Open Access
33 Citations
7,377 Views
15 Pages

Synthesis and Biological Evaluation of RGD–Cryptophycin Conjugates for Targeted Drug Delivery

  • Adina Borbély,
  • Eduard Figueras,
  • Ana Martins,
  • Simone Esposito,
  • Giulio Auciello,
  • Edith Monteagudo,
  • Annalise Di Marco,
  • Vincenzo Summa,
  • Paola Cordella and
  • Norbert Sewald
  • + 5 authors

Cryptophycins are potent tubulin polymerization inhibitors with picomolar antiproliferative potency in vitro and activity against multidrug-resistant (MDR) cancer cells. Because of neurotoxic side effects and limited efficacy in vivo, cryptophycin-52...

  • Article
  • Open Access
17 Citations
5,849 Views
17 Pages

The protein therapeutic and CD95L inhibitor asunercept is currently under clinical investigation for the treatment of glioblastoma and myelodysplastic syndrome. The purpose of this study was to predict the asunercept pharmacokinetics in children and...

  • Article
  • Open Access
20 Citations
5,630 Views
10 Pages

Simulation of Airway Deposition of an Aerosol Drug in COPD Patients

  • Árpád Farkas,
  • Frantisek Lizal,
  • Jan Jedelsky,
  • Jakub Elcner,
  • Alpár Horváth and
  • Miroslav Jicha

Medical aerosols are key elements of current chronic obstructive pulmonary disease (COPD) therapy. Therapeutic effects are conditioned by the delivery of the right amount of medication to the right place within the airways, that is, to the drug recep...

  • Article
  • Open Access
13 Citations
5,994 Views
20 Pages

The aim of the present study was to develop an alternative process to spray granulation in order to prepare high loaded spherical nicotinamide (NAM) pellets by wet extrusion and spheronisation. Therefore, a quality by design approach was implemented...

  • Article
  • Open Access
26 Citations
4,852 Views
17 Pages

Electrospun xanthan polysaccharide nanofibers (X) were developed as an encapsulation and delivery system of the poorly absorbed polyphenol compounds, gallic acid (GA) and (−)-epigallocatechin gallate (EGCG). Scanning electron microscopy was use...

  • Article
  • Open Access
208 Citations
15,779 Views
17 Pages

3D Printed Pellets (Miniprintlets): A Novel, Multi-Drug, Controlled Release Platform Technology

  • Atheer Awad,
  • Fabrizio Fina,
  • Sarah J. Trenfield,
  • Pavanesh Patel,
  • Alvaro Goyanes,
  • Simon Gaisford and
  • Abdul W. Basit

Selective laser sintering (SLS) is a single-step three-dimensional printing (3DP) process that can be leveraged to engineer a wide array of drug delivery systems. The aim of this work was to utilise SLS 3DP, for the first time, to produce small oral...

  • Review
  • Open Access
15 Citations
11,826 Views
19 Pages

Oral solid drug formulation is the most common route for administration and it is vital to increase knowledge of the gastrointestinal physiological environment to understand dissolution and absorption processes and to develop reliable biorelevant in...

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Pharmaceutics - ISSN 1999-4923