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Pharmaceutics, Volume 12, Issue 1

2020 January - 85 articles

Cover Story: Polymeric microcontainers loaded with insulin, a permeation enhancer, and a protease inhibitor are placed with collective unidirectional release towards a Caco-2 monolayer for in vitro insulin proteolysis and permeation studies. The powder formulation loaded in the microcontainers is further optimized on the basis of ex vivo insulin permeation studies across porcine intestinal tissue in a Franz diffusion cell setup. Finally, enteric coating of microcontainers followed by loading into size 9 gelatin capsules enables investigation of the in vivo performance regarding increasing insulin bioavailability upon oral gavage. View this paper.
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Articles (85)

  • Article
  • Open Access
60 Citations
5,829 Views
24 Pages

Mechanism and Improved Dissolution of Glycyrrhetinic Acid Solid Dispersion by Alkalizers

  • Luning Dong,
  • Yaping Mai,
  • Qiang Liu,
  • Wannian Zhang and
  • Jianhong Yang

The purpose of this study was to increase the dissolution of glycyrrhetinic acid (GA) by preparing ternary solid dispersion (TSD) systems containing alkalizers, and to explore the modulating mechanism of alkalizers in solid dispersion systems. GA TSD...

  • Review
  • Open Access
129 Citations
12,369 Views
28 Pages

Bone diseases, such as bone cancer, bone infection and osteoporosis, constitute a major issue for modern societies as a consequence of their progressive ageing. Even though these pathologies can be currently treated in the clinic, some of those treat...

  • Article
  • Open Access
5 Citations
4,118 Views
14 Pages

In this study, we established a robust feed-forward control model for the tableting process by partial least squares regression using the near-infrared (NIR) spectra and physical attributes of the granules to be compressed. The NIR spectra of granule...

  • Article
  • Open Access
14 Citations
3,705 Views
14 Pages

Naturally sourced products introduced to human nutrition and rediscovered for therapy include polysaccharides from potatoes. The starch may obtain unique properties via acetylation with acetic anhydride at 13 cm3/100 g of starch as the basic dose of...

  • Article
  • Open Access
28 Citations
8,009 Views
11 Pages

Gastrointestinal Tracking and Gastric Emptying of Coated Capsules in Rats with or without Sedation Using CT imaging

  • Noemí Gómez-Lado,
  • Iria Seoane-Viaño,
  • Silvia Matiz,
  • Christine M. Madla,
  • Vipul Yadav,
  • Pablo Aguiar,
  • Abdul W. Basit and
  • Alvaro Goyanes

Following oral administration, gastric emptying is often a rate-limiting step in the absorption of drugs and is dependent on both physiological and pharmaceutical factors. To guide translation into humans, small animal imaging during pre-clinical stu...

  • Article
  • Open Access
16 Citations
5,160 Views
23 Pages

Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules

  • Cecilia B. Michalowski,
  • Marcelo D. Arbo,
  • Louise Altknecht,
  • Andréia N. Anciuti,
  • Angélica S. G. Abreu,
  • Luciana M. R. Alencar,
  • Adriana R. Pohlmann,
  • Solange C. Garcia and
  • Sílvia S. Guterres

Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimo...

  • Article
  • Open Access
68 Citations
6,624 Views
14 Pages

Comparison of Various Cell Lines and Three-Dimensional Mucociliary Tissue Model Systems to Estimate Drug Permeability Using an In Vitro Transport Study to Predict Nasal Drug Absorption in Rats

  • Tomoyuki Furubayashi,
  • Daisuke Inoue,
  • Noriko Nishiyama,
  • Akiko Tanaka,
  • Reiko Yutani,
  • Shunsuke Kimura,
  • Hidemasa Katsumi,
  • Akira Yamamoto and
  • Toshiyasu Sakane

Recently, various types of cultured cells have been used to research the mechanisms of transport and metabolism of drugs. Although many studies using cultured cell systems have been published, a comparison of different cultured cell systems has never...

  • Article
  • Open Access
7 Citations
4,464 Views
10 Pages

We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization. The goal of the present work was to further elaborate...

  • Article
  • Open Access
28 Citations
5,044 Views
12 Pages

Induction of WNT16 via Peptide-mRNA Nanoparticle-Based Delivery Maintains Cartilage Homeostasis

  • Huimin Yan,
  • Ying Hu,
  • Antonina Akk,
  • Muhammad Farooq Rai,
  • Hua Pan,
  • Samuel A. Wickline and
  • Christine T.N. Pham

Osteoarthritis (OA) is a progressive joint disease that causes significant disability and pain and for which there are limited treatment options. We posit that delivery of anabolic factors that protect and maintain cartilage homeostasis will halt or...

  • Article
  • Open Access
75 Citations
8,260 Views
11 Pages

PLGA-PEG-ANG-2 Nanoparticles for Blood–Brain Barrier Crossing: Proof-of-Concept Study

  • Gina P. Hoyos-Ceballos,
  • Barbara Ruozi,
  • Ilaria Ottonelli,
  • Federica Da Ros,
  • Maria Angela Vandelli,
  • Flavio Forni,
  • Eleonora Daini,
  • Antonietta Vilella,
  • Michele Zoli and
  • Betty L. López-Osorio
  • + 2 authors

The treatment of diseases that affect the central nervous system (CNS) represents a great research challenge due to the restriction imposed by the blood–brain barrier (BBB) to allow the passage of drugs into the brain. However, the use of modif...

  • Article
  • Open Access
58 Citations
15,586 Views
28 Pages

A Mechanistic Physiologically-Based Biopharmaceutics Modeling (PBBM) Approach to Assess the In Vivo Performance of an Orally Administered Drug Product: From IVIVC to IVIVP

  • Marival Bermejo,
  • Bart Hens,
  • Joseph Dickens,
  • Deanna Mudie,
  • Paulo Paixão,
  • Yasuhiro Tsume,
  • Kerby Shedden and
  • Gordon L. Amidon

The application of in silico modeling to predict the in vivo outcome of an oral drug product is gaining a lot of interest. Fully relying on these models as a surrogate tool requires continuous optimization and validation. To do so, intraluminal and s...

  • Article
  • Open Access
20 Citations
3,992 Views
13 Pages

Optimization of Rifapentine-Loaded Lipid Nanoparticles Using a Quality-by-Design Strategy

  • Joana Magalhães,
  • Luise L. Chaves,
  • Alexandre C. Vieira,
  • Susana G. Santos,
  • Marina Pinheiro and
  • Salette Reis

This work aims to optimize and assess the potential use of lipid nanoparticles, namely nanostructured lipid carriers (NLCs), as drug delivery systems of rifapentine (RPT) for the treatment of tuberculosis (TB). A Box–Behnken design was used to...

  • Article
  • Open Access
31 Citations
4,715 Views
22 Pages

Novel Intranasal Drug Delivery: Geraniol Charged Polymeric Mixed Micelles for Targeting Cerebral Insult as a Result of Ischaemia/Reperfusion

  • Sara M. Soliman,
  • Nermin M. Sheta,
  • Bassant M. M. Ibrahim,
  • Mohammad M. El-Shawwa and
  • Shady M. Abd El-Halim

Brain damage caused by cerebral ischaemia/reperfusion (I/R) can lead to handicapping. So, the present study aims to evaluate the prophylactic and therapeutic effects of geraniol in the form of intranasal polymeric mixed micelle (PMM) on the central n...

  • Article
  • Open Access
96 Citations
8,133 Views
16 Pages

This work presents a novel approach for producing gastro-retentive floating tablets (GRFT) by coupling hot-melt extrusion (HME) and fused deposition three-dimensional printing (3DP). Filaments containing theophylline (THEO) within a hydroxypropyl cel...

  • Article
  • Open Access
12 Citations
9,845 Views
11 Pages

Inhalation therapy with a nebulizer is widely used in chronic respiratory disease. Mixing inhalation solutions/suspensions for simultaneous inhalation is more convenient and might simplify the administration procedure. However, there are no data avai...

  • Article
  • Open Access
56 Citations
7,605 Views
28 Pages

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

  • Khaled AbouAitah,
  • Agata Stefanek,
  • Iman M. Higazy,
  • Magdalena Janczewska,
  • Anna Swiderska-Sroda,
  • Agnieszka Chodara,
  • Jacek Wojnarowicz,
  • Urszula Szałaj,
  • Samar A. Shahein and
  • Witold Lojkowski
  • + 4 authors

Targeted drug delivery offers great opportunities for treating cancer. Here, we developed a novel anticancer targeted delivery system for piperine (Pip), an alkaloid prodrug derived from black pepper that exhibits anticancer effects. The tailored del...

  • Article
  • Open Access
33 Citations
5,175 Views
14 Pages

Controlling metastasis is an important strategy in cancer treatment. Nanotechnology and nucleic acids with novel modalities are promising regulators of cancer metastasis. We aimed to develop a small interfering RNA (siRNA) systemic delivery and anti-...

  • Review
  • Open Access
22 Citations
4,654 Views
23 Pages

Antitumor Features of Vegetal Protein-Based Nanotherapeutics

  • Silvia Voci,
  • Agnese Gagliardi,
  • Massimo Fresta and
  • Donato Cosco

The introduction of nanotechnology into pharmaceutical application revolutionized the administration of antitumor drugs through the modulation of their accumulation in specific organs/body compartments, a decrease in their side-effects and their cont...

  • Article
  • Open Access
29 Citations
6,155 Views
18 Pages

Today, probiotics are predominantly used in liquid or semi-solid functionalized foods, showing a rapid loss of cell viability. Due to the increasing spread of antibiotic resistance, probiotics are promising in pharmaceutical development because of th...

  • Article
  • Open Access
14 Citations
5,139 Views
11 Pages

Continuous manufacturing (CM) is a promising strategy to achieve various benefits in the context of quality, flexibility, safety and cost in pharmaceutical production. One of the main technical challenges of CM is that the process needs to handle tra...

  • Article
  • Open Access
12 Citations
5,371 Views
22 Pages

Focused ultrasound (FUS) coupled with microbubbles (MB) has been found to be a promising approach to disrupt the blood-brain barrier (BBB). However, how this disruption affects drug transport remains unclear. In this study, drug transport in combinat...

  • Review
  • Open Access
265 Citations
27,079 Views
20 Pages

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

  • Sang Hoon Lee,
  • Rajiv Bajracharya,
  • Jeong Youn Min,
  • Ji-Won Han,
  • Byeong Ju Park and
  • Hyo-Kyung Han

Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable...

  • Review
  • Open Access
44 Citations
7,879 Views
22 Pages

Antibodies for the Treatment of Brain Metastases, a Dream or a Reality?

  • Marco Cavaco,
  • Diana Gaspar,
  • Miguel ARB Castanho and
  • Vera Neves

The incidence of brain metastases (BM) in cancer patients is increasing. After diagnosis, overall survival (OS) is poor, elicited by the lack of an effective treatment. Monoclonal antibody (mAb)-based therapy has achieved remarkable success in treati...

  • Article
  • Open Access
122 Citations
12,001 Views
15 Pages

3D Printing of Drug-Loaded Thermoplastic Polyurethane Meshes: A Potential Material for Soft Tissue Reinforcement in Vaginal Surgery

  • Juan Domínguez-Robles,
  • Caterina Mancinelli,
  • Elena Mancuso,
  • Inmaculada García-Romero,
  • Brendan F. Gilmore,
  • Luca Casettari,
  • Eneko Larrañeta and
  • Dimitrios A. Lamprou

Current strategies to treat pelvic organ prolapse (POP) or stress urinary incontinence (SUI), include the surgical implantation of vaginal meshes. Recently, there have been multiple reports of issues generated by these meshes conventionally made of p...

  • Article
  • Open Access
10 Citations
4,352 Views
16 Pages

Zein Beta-Cyclodextrin Micropowders for Iron Bisglycinate Delivery

  • Diletta Esposito,
  • Giovanni Dal Poggetto,
  • Aurélie Demont,
  • Nicolai Kraut,
  • Agnese Miro,
  • Francesca Ungaro,
  • Paola Laurienzo and
  • Fabiana Quaglia

Given the limited number of materials available to design delivery platforms for nutrients, the rational combination of raw materials already approved as food ingredients and their processing through nano-micro technology can offer a unique tool for...

  • Article
  • Open Access
12 Citations
5,388 Views
10 Pages

Energy Transfer in Vials Nested in a Rack System During Lyophilization

  • Sarah Daller,
  • Wolfgang Friess and
  • Rudolf Schroeder

Small batch sizes are a consequence of more personalized medicine and reflect a trend in the biopharmaceutical industry. Freeze drying of vials nested in a rack system is a tool used in new flexible pilot scale processing lines. Understanding of heat...

  • Article
  • Open Access
16 Citations
4,429 Views
18 Pages

Polymer Cancerostatics Containing Cell-Penetrating Peptides: Internalization Efficacy Depends on Peptide Type and Spacer Length

  • Eliška Böhmová,
  • Robert Pola,
  • Michal Pechar,
  • Jozef Parnica,
  • Daniela Machová,
  • Olga Janoušková and
  • Tomáš Etrych

Cell-penetrating peptides (CPPs) are commonly used substances enhancing the cellular uptake of various cargoes that do not easily cross the cellular membrane. CPPs can be either covalently bound directly to the cargo or they can be attached to a tran...

  • Article
  • Open Access
19 Citations
6,949 Views
14 Pages

Stability and Compatibility Studies of Levothyroxine Sodium in Solid Binary Systems—Instrumental Screening

  • Ionuț Ledeți,
  • Mirabela Romanescu,
  • Denisa Cîrcioban,
  • Adriana Ledeți,
  • Gabriela Vlase,
  • Titus Vlase,
  • Oana Suciu,
  • Marius Murariu,
  • Sorin Olariu and
  • Doina Piciu
  • + 2 authors

The influence of excipients on the stability of sodium levothyroxine pentahydrate (LTSS) under ambient conditions and thermal stress was evaluated. Since LTSS is a synthetic hormone with a narrow therapeutic index, the interactions of LTSS with excip...

  • Article
  • Open Access
27 Citations
4,828 Views
17 Pages

Insight into the Formation of Glimepiride Nanocrystals by Wet Media Milling

  • Djordje Medarević,
  • Svetlana Ibrić,
  • Elisavet Vardaka,
  • Miodrag Mitrić,
  • Ioannis Nikolakakis and
  • Kyriakos Kachrimanis

Nanocrystal formation for the dissolution enhancement of glimepiride was attempted by wet media milling. Different stabilizers were tested and the obtained nanosuspensions were solidified by spray drying in presence of mannitol, and characterized reg...

  • Article
  • Open Access
37 Citations
5,032 Views
13 Pages

Novel Population Pharmacokinetic Model for Linezolid in Critically Ill Patients and Evaluation of the Adequacy of the Current Dosing Recommendation

  • Amaia Soraluce,
  • Helena Barrasa,
  • Eduardo Asín-Prieto,
  • Jose Ángel Sánchez-Izquierdo,
  • Javier Maynar,
  • Arantxazu Isla and
  • Alicia Rodríguez-Gascón

Antimicrobial treatment in critically ill patients remains challenging. The aim of this study was to develop a population pharmacokinetic model for linezolid in critically ill patients and to evaluate the adequacy of current dosing recommendation (60...

  • Review
  • Open Access
131 Citations
12,058 Views
21 Pages

Although dry powder inhalers (DPIs) have attracted great interest compared to nebulizers and metered-dose inhalers (MDIs), drug deposition in the deep lung is still insufficient to enhance therapeutic activity. Indeed, it is estimated that only 10&nd...

  • Article
  • Open Access
110 Citations
11,804 Views
23 Pages

Development of Bio-Active Patches Based on Pectin for the Treatment of Ulcers and Wounds Using 3D-Bioprinting Technology

  • Eleftherios G. Andriotis,
  • Georgios K. Eleftheriadis,
  • Christina Karavasili and
  • Dimitrios G. Fatouros

Biodegradable 3D-printable inks based on pectin have been developed as a system for direct and indirect wound-dressing applications, suitable for 3D printing technologies. The 3D-printable inks formed free-standing transparent films upon drying, with...

  • Article
  • Open Access
152 Citations
12,283 Views
13 Pages

This study was performed to develop novel core-shell gastroretentive floating pulsatile drug delivery systems using a hot-melt extrusion-paired fused deposition modeling (FDM) 3D printing and direct compression method. Hydroxypropyl cellulose (HPC) a...

  • Article
  • Open Access
30 Citations
7,225 Views
14 Pages

In Vitro, Ex Vivo and In Vivo Evaluation of Microcontainers for Oral Delivery of Insulin

  • Jacob Rune Jørgensen,
  • Feiyang Yu,
  • Ramakrishnan Venkatasubramanian,
  • Line Hagner Nielsen,
  • Hanne Mørck Nielsen,
  • Anja Boisen,
  • Thomas Rades and
  • Anette Müllertz

Enhancing the oral bioavailability of peptides has received a lot of attention for decades but remains challenging, partly due to low intestinal membrane permeability. Combining a permeation enhancer (PE) with unidirectionally releasing microcontaine...

  • Article
  • Open Access
15 Citations
4,147 Views
12 Pages

Extended Intake of Mulberry Leaf Extract Delayed Metformin Elimination via Inhibiting the Organic Cation Transporter 2

  • Hyun Wook Huh,
  • Young-Guk Na,
  • Ki-Hyun Bang,
  • Sung-Jin Kim,
  • Minki Kim,
  • Kyung-Tae Kim,
  • Jong-Seong Kang,
  • Young-Ho Kim,
  • Jong-Suep Baek and
  • Cheong-Weon Cho
  • + 1 author

Diabetes mellitus (DM) has become a major health problem in most countries of the world. DM causes many complications, including hyperglycemia, diabetic ketoacidosis, and death. In Asia, mulberry has been used widely in the treatment of DM. Combinati...

  • Review
  • Open Access
2 Citations
4,103 Views
20 Pages

The biosensing platform is noteworthy for high sensitivity and precise detection of target analytes, which are related to the status of cells or specific diseases. The modification of the transducers with metallic nanoparticles (MNPs) has attracted a...

  • Article
  • Open Access
40 Citations
5,215 Views
23 Pages

Clay-Polymer Nanocomposites Prepared by Reactive Melt Extrusion for Sustained Drug Release

  • Xu Liu,
  • Xingyu Lu,
  • Yongchao Su,
  • Eucharist Kun and
  • Feng Zhang

Clay–polymer nanocomposites have exhibited a great potential as carriers for controlled release drug delivery. This study aims to prepare exfoliated montmorillonite–Eudragit RS nanocomposites using reactive melt extrusion and investigate...

  • Article
  • Open Access
16 Citations
7,297 Views
17 Pages

Effect of Formulation Factors and Oxygen Levels on the Stability of Aqueous Injectable Solution Containing Pemetrexed

  • Dong Han Won,
  • Heejun Park,
  • Eun-Sol Ha,
  • Yong Min Kim,
  • Hyung Don Hwang,
  • Sun Woo Jang and
  • Min-Soo Kim

The aim of this study was to investigate the effects of various parameters at each control strategy in drug product degradation on the stability of pemetrexed in injectable aqueous solution. A forced degradation study confirmed that oxidation is the...

  • Article
  • Open Access
21 Citations
4,302 Views
14 Pages

With the development of modern medical technology, common diseases usually can be treated by traditional medicines and their formulation, while diseases with multiple etiologies still remain a great challenge in clinic. Nanoformulation was widely exp...

  • Review
  • Open Access
18 Citations
9,735 Views
16 Pages

Purpose: To review in vitro testing and simulation platforms that are in current use to predict in vivo performances of generic products as well as other situations to provide evidence for biowaiver and support drug formulations development. Methods:...

  • Article
  • Open Access
23 Citations
5,667 Views
19 Pages

Hyaluronate Nanoparticles as a Delivery System to Carry Neuroglobin to the Brain after Stroke

  • Santos Blanco,
  • Sebastián Peralta,
  • María Encarnación Morales,
  • Esther Martínez-Lara,
  • José Rafael Pedrajas,
  • Herminia Castán,
  • María Ángeles Peinado and
  • María Adolfina Ruiz

Therapies against stroke can restore the blood supply but cannot prevent the ischemic damage nor stimulate the recovery of the infarcted zone. The neuroglobin protein plays an important role in the neuro-regeneration process after stroke; however, th...

  • Article
  • Open Access
65 Citations
4,662 Views
18 Pages

Molecularly Imprinted Polymers (MIPs) as Theranostic Systems for Sunitinib Controlled Release and Self-Monitoring in Cancer Therapy

  • Ortensia Ilaria Parisi,
  • Mariarosa Ruffo,
  • Rocco Malivindi,
  • Anna Francesca Vattimo,
  • Vincenzo Pezzi and
  • Francesco Puoci

Cytotoxic agents that are used conventionally in cancer therapy present limitations that affect their efficacy and safety profile, leading to serious adverse effects. In the aim to overcome these drawbacks, different approaches have been investigated...

  • Article
  • Open Access
12 Citations
3,119 Views
11 Pages

In this study, the rapid expansion of the supercritical solutions (RESS) process was used to produce microparticles of a commonly used anti-inflammatory drug, ethenzamide. The effects of process parameters in RESS including the extraction temperature...

  • Article
  • Open Access
80 Citations
5,786 Views
18 Pages

Selenium nanoparticles (SeNPs) have attracted attention due to their favorable properties, unique bioactivities, and potential for use in nutritional supplements and nanomedicine applications. However, the application of SeNPs in the clinic has been...

  • Review
  • Open Access
117 Citations
13,854 Views
23 Pages

Patient Centric Pharmaceutical Drug Product Design—The Impact on Medication Adherence

  • Enrica Menditto,
  • Valentina Orlando,
  • Giuseppe De Rosa,
  • Paola Minghetti,
  • Umberto Maria Musazzi,
  • Caitriona Cahir,
  • Marta Kurczewska-Michalak,
  • Przemysław Kardas,
  • Elísio Costa and
  • Isabel F Almeida
  • + 1 author

Medication adherence is a growing concern for public health and poor adherence to therapy has been associated with poor health outcomes and higher costs for patients. Interventions for improving adherence need to consider the characteristics of the i...

  • Article
  • Open Access
10 Citations
4,876 Views
10 Pages

Recent studies have shown that β2-Adrenoreceptor is a regulator of the a-synuclein gene driving risk of Parkinson’s disease. The β2-AR agonist (R)-salbutamol, eutomer of rac-salbutamol, may hold therapeutic potential for Parkinson&rsq...

  • Article
  • Open Access
19 Citations
4,542 Views
16 Pages

This study optimized the preparation of electrosprayed microspheres containing leuprolide and developed an in vitro–in vivo correlation (IVIVC) model that enables mutual prediction between in vitro and in vivo dissolution. The pharmacokinetic (...

  • Article
  • Open Access
12 Citations
9,079 Views
21 Pages

Reactive impurities originating from excipients can cause drug stability issues, even at trace amounts. When produced during final dosage form storage, they are especially hard to control, and often, factors inducing their formation remain unidentifi...

  • Article
  • Open Access
58 Citations
6,003 Views
25 Pages

Docetaxel-Loaded Disulfide Cross-Linked Nanoparticles Derived from Thiolated Sodium Alginate for Colon Cancer Drug Delivery

  • Hock Ing Chiu,
  • Asila Dinie Ayub,
  • Siti Nur Aishah Mat Yusuf,
  • Noorfatimah Yahaya,
  • Erazuliana Abd Kadir and
  • Vuanghao Lim

In this study, fluorescein-labelled wheat germ agglutinin (fWGA)-conjugated disulfide cross-linked sodium alginate nanoparticles were developed to specifically target docetaxel (DTX) to colon cancer cells. Different amounts of 3-mercaptopropionic aci...

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Pharmaceutics - ISSN 1999-4923