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485 Results Found

  • Article
  • Open Access
54 Citations
6,374 Views
13 Pages

Electrospun Coaxial Fibers to Optimize the Release of Poorly Water-Soluble Drug

  • Yubo Liu,
  • Xiaohong Chen,
  • Yuyang Liu,
  • Yuhang Gao and
  • Ping Liu

24 January 2022

In a drug delivery system, the physicochemical properties of the polymeric matrix have a positive impact on the bioavailability of poorly water-soluble drugs. In this work, monolithic F1 fibers and coaxial F2 fibers were successfully prepared using p...

  • Review
  • Open Access
81 Citations
6,279 Views
14 Pages

Nanoconjugations have been demonstrated to be a dominant strategy for drug delivery and biomedical applications. In this review, we intend to describe several strategies for drug formulation, especially to improve the bioavailability of poorly water-...

  • Article
  • Open Access
25 Citations
6,687 Views
17 Pages

Formulation of Orally Disintegrating Films as an Amorphous Solid Solution of a Poorly Water-Soluble Drug

  • Pattaraporn Panraksa,
  • Pratchaya Tipduangta,
  • Kittisak Jantanasakulwong and
  • Pensak Jantrawut

27 November 2020

The objective of the present study was to develop an orally disintegrating film (ODF) for a poorly water-soluble drug, phenytoin (PHT), using the cosolvent solubilization technique to achieve the amorphization of the drug, followed by the preparation...

  • Article
  • Open Access
3 Citations
2,535 Views
12 Pages

Preclinical Bioavailability Assessment of a Poorly Water-Soluble Drug, HGR4113, Using a Stable Isotope Tracer

  • Eun Ji Ha,
  • Jeong In Seo,
  • Shaheed Ur Rehman,
  • Hyung Soon Park,
  • Sang-Ku Yoo and
  • Hye Hyun Yoo

Drug solubility limits intravenous dosing for poorly water-soluble medicines, which misrepresents their bioavailability estimation. The current study explored a method using a stable isotope tracer to assess the bioavailability of drugs that are poor...

  • Article
  • Open Access
73 Citations
7,712 Views
16 Pages

Amorphous solid dispersions (ASDs) improve the oral delivery of poorly water-soluble drugs. ASDs of olanzapine (OLZ), which have a high melting point and low solubility, are performed using a complicated process. Three-dimensional (3D) printing based...

  • Article
  • Open Access
19 Citations
5,652 Views
20 Pages

The aim of the study was to develop a novel buccal dosage form to transport rhodamine 123 and human insulin as models for poorly water-soluble and biological drugs, using lipid-core micelles (LCMs)-loaded mucoadhesive films. LCMs were synthesized by...

  • Article
  • Open Access
3 Citations
2,687 Views
17 Pages

Physicochemical Properties, Drug Release and In Situ Depot-Forming Behaviors of Alginate Hydrogel Containing Poorly Water-Soluble Aripiprazole

  • Hy D. Nguyen,
  • Munsik Jang,
  • Hai V. Ngo,
  • Myung-Chul Gil,
  • Gang Jin,
  • Jing-Hao Cui,
  • Qing-Ri Cao and
  • Beom-Jin Lee

29 November 2024

The objective of this study was to investigate the physicochemical properties, drug release and in situ depot-forming behavior of alginate hydrogel containing poorly water-soluble aripiprazole (ARP) for achieving free-flowing injectability, clinicall...

  • Review
  • Open Access
224 Citations
21,198 Views
33 Pages

Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especia...

  • Review
  • Open Access
49 Citations
5,286 Views
12 Pages

Physicochemical characterization is a crucial step for the successful development of solid dispersions, including the determination of drug crystallinity and molecular interactions. Typically, the detection of molecular interactions will assist in th...

  • Review
  • Open Access
6 Citations
5,327 Views
26 Pages

The solubility behavior of drugs is a critical factor in formulation development. Approximately 40–45% of new drugs face market entry challenges due to low water solubility. Enhancing drug bioavailability is thus essential in developing pharmac...

  • Review
  • Open Access
1 Citations
696 Views
42 Pages

Background/Objectives: The poor aqueous solubility of many therapeutic compounds remains a key barrier to achieving optimal oral bioavailability. While traditional formulation strategies—such as surfactant-based solubilization, nanocrystals, an...

  • Review
  • Open Access
33 Citations
6,405 Views
31 Pages

Cancer is one of the leading causes of death worldwide. In the available treatments, chemotherapy is one of the most used, but has several associated problems, namely the high toxicity to normal cells and the resistance acquired by cancer cells to th...

  • Feature Paper
  • Article
  • Open Access
12 Citations
6,406 Views
16 Pages

2 December 2021

Itraconazole (ITZ) is a class II drug according to the biopharmaceutical classification system. Its solubility is pH 3-dependent, and it is poorly water-soluble. Its pKa is 3.7, which makes it a weak base drug. The aim of this study was to prepare so...

  • Article
  • Open Access
4 Citations
3,242 Views
13 Pages

Hydroxyapatite Nanorods Based Drug Delivery Systems for Bumetanide and Meloxicam, Poorly Water Soluble Active Principles

  • Valeria Friuli,
  • Lauretta Maggi,
  • Giovanna Bruni,
  • Francesca Caso and
  • Marcella Bini

2 January 2024

Poorly water-soluble drugs represent a challenge for the pharmaceutical industry because it is necessary to find properly tuned and efficient systems for their release. In this framework, organic–inorganic hybrid systems could represent a promi...

  • Review
  • Open Access
27 Citations
6,837 Views
30 Pages

Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability

  • Arif Budiman,
  • Eli Lailasari,
  • Neng Vera Nurani,
  • Ellen Nathania Yunita,
  • Gracia Anastasya,
  • Rizqa Nurul Aulia,
  • Ira Novianty Lestari,
  • Laila Subra and
  • Diah Lia Aulifa

The prevalence of active pharmaceutical ingredients (APIs) with low water solubility has experienced a significant increase in recent years. These APIs present challenges in formulation, particularly for oral dosage forms, despite their considerable...

  • Article
  • Open Access
19 Citations
4,759 Views
13 Pages

Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib

  • Yong-Han Kim,
  • Seong-Bo Kim,
  • Se-Hee Choi,
  • Thi-Thao-Linh Nguyen,
  • Sung-Hoon Ahn,
  • Kyung-Sun Moon,
  • Kwan-Hyung Cho,
  • Tae-Yong Sim,
  • Eun-Ji Heo and
  • Dong-Jin Jang
  • + 4 authors

The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-su...

  • Article
  • Open Access
9 Citations
3,233 Views
22 Pages

The poor bioavailability of many newly developed active pharmaceutical ingredients (APIs) poses a major challenge in formulation development. To overcome this issue, strategies such as the preparation of amorphous solid dispersions (ASDs), and the ap...

  • Article
  • Open Access
35 Citations
7,828 Views
12 Pages

The objective of this study is to develop suitable formulations to improve the dissolution rate of poorly water soluble drugs. We selected lipid-based formulation as a drug carrier and modified the surface using positively charged chitosan derivative...

  • Article
  • Open Access
8 Citations
2,668 Views
20 Pages

Twin Screw Melt Granulation of Simvastatin: Drug Solubility and Dissolution Rate Enhancement Using Polymer Blends

  • Rasha M. Elkanayati,
  • Indrajeet Karnik,
  • Prateek Uttreja,
  • Nagarjuna Narala,
  • Sateesh Kumar Vemula,
  • Krizia Karry and
  • Michael A. Repka

Background/Objectives: This study evaluates the efficacy of twin screw melt granulation (TSMG), and hot-melt extrusion (HME) techniques in enhancing the solubility and dissolution of simvastatin (SIM), a poorly water-soluble drug with low bioavailabi...

  • Article
  • Open Access
15 Citations
4,060 Views
19 Pages

We investigated the solubility–permeability interplay using a solubilizer additive under non-sink conditions. Sodium lauryl sulfate (SLS) was used as a solubilizer additive. The solubility and permeability of two poorly soluble drugs at various doses...

  • Article
  • Open Access
18 Citations
7,746 Views
40 Pages

Exploring Deep Eutectic Solvents as Pharmaceutical Excipients: Enhancing the Solubility of Ibuprofen and Mefenamic Acid

  • Mihaela-Alexandra Nica,
  • Valentina Anuța,
  • Cristian Andi Nicolae,
  • Lăcrămioara Popa,
  • Mihaela Violeta Ghica,
  • Florentina-Iuliana Cocoș and
  • Cristina-Elena Dinu-Pîrvu

2 October 2024

Objectives: The study explores the potential of various deep eutectic solvents (DESs) to serve as drug delivery systems and pharmaceutical excipients. The research focuses on two primary objectives: evaluating the ability of the selected DES systems...

  • Article
  • Open Access
21 Citations
3,851 Views
14 Pages

Supercritical Solvent Impregnation of Different Drugs in Mesoporous Nanostructured ZnO

  • Mauro Banchero,
  • Sara S. Y. Mohamed,
  • Federica Leone,
  • Francesca Lopez,
  • Silvia Ronchetti,
  • Luigi Manna and
  • Barbara Onida

Supercritical solvent impregnation (SSI) is a green unconventional technique for preparing amorphous drug formulations. A mesoporous nanostructured ZnO (mesoNsZnO) carrier with 8-nm pores, spherical-nanoparticle morphology, and an SSA of 75 m2/g has...

  • Article
  • Open Access
31 Citations
7,021 Views
16 Pages

Investigation of Crystallization and Salt Formation of Poorly Water-Soluble Telmisartan for Enhanced Solubility

  • Chulhun Park,
  • Nileshkumar M. Meghani,
  • Yongkwan Shin,
  • Euichaul Oh,
  • Jun-Bom Park,
  • Jing-Hao Cui,
  • Qing-Ri Cao,
  • Thao Truong-Dinh Tran,
  • Phuong Ha-Lien Tran and
  • Beom-Jin Lee

The crystal changes and salt formation of poorly water-soluble telmisartan (TEL) in various solvents were investigated for enhanced solubility, stability and crystallinity. Polymorphic behaviors of TEL were characterized by dispersing in distilled wa...

  • Article
  • Open Access
5 Citations
5,519 Views
21 Pages

21 March 2024

The aim of this study was to determine the drug loading capacity of phosphatidylcholine-based formulations for four poorly water-soluble drug substances (clofazimine, fenofibrate, artemether, cannabidiol). Two self-dispersing lipid formulations were...

  • Article
  • Open Access
8 Citations
3,376 Views
12 Pages

Fabrication of Submicrometer-Sized Meloxicam Particles Using Femtosecond Laser Ablation in Gas and Liquid Environments

  • Eszter Nagy,
  • Attila Andrásik,
  • Tamás Smausz,
  • Tibor Ajtai,
  • Fruzsina Kun-Szabó,
  • Judit Kopniczky,
  • Zoltán Bozóki,
  • Piroska Szabó-Révész,
  • Rita Ambrus and
  • Béla Hopp

13 April 2021

In pharmaceutical development, more and more drugs are classified as poorly water-soluble or insoluble. Particle size reduction is a common way to fight this trend by improving dissolution rate, transport characteristics and bioavailability. Pulsed l...

  • Review
  • Open Access
16 Citations
9,076 Views
35 Pages

Amorphous Solid Dispersion as Drug Delivery Vehicles in Cancer

  • Arif Budiman,
  • Annisa Luthfiyah Handini,
  • Mutia Nur Muslimah,
  • Neng Vera Nurani,
  • Eli Laelasari,
  • Insan Sunan Kurniawansyah and
  • Diah Lia Aulifa

11 August 2023

Cancer treatment has improved over the past decades, but a major challenge lies in drug formulation, specifically for oral administration. Most anticancer drugs have poor water solubility which can affect their bioavailability. This causes suboptimal...

  • Article
  • Open Access
39 Citations
6,161 Views
25 Pages

Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as l...

  • Article
  • Open Access
562 Views
18 Pages

Selection of Solubility Enhancement Technologies for S-892216, a Novel COVID-19 Drug Candidate

  • Ryo Ohashi,
  • Shuichi Otake,
  • Tatsuhiko Murata,
  • Ryosuke Watari,
  • Shinpei Yoshida,
  • Mikiko Kitade,
  • Daisuke Kondo and
  • Go Kimura

Background/Objectives: S-892216 is a poorly water-soluble drug developed as a novel oral treatment for COVID-19, although its oral absorption is low. For Phase 1 (Ph1) studies and commercial use, both oral solution and solid dispersion technologies a...

  • Article
  • Open Access
28 Citations
4,560 Views
16 Pages

Enlarged Pore Size Chiral Mesoporous Silica Nanoparticles Loaded Poorly Water-Soluble Drug Perform Superior Delivery Effect

  • Yingyu Guo,
  • Kaijun Gou,
  • Baixue Yang,
  • Yumei Wang,
  • Xueyu Pu,
  • Sanming Li and
  • Heran Li

30 September 2019

Large mesopores of chiral silica nanoparticles applied as drug carrier are worth studying. In this study, chiral mesoporous silica nanoparticles (CMSN) and enlarged chiral mesoporous silica nanoparticles (E-CMSN) with a particle size from 200 to 300...

  • Article
  • Open Access
5 Citations
3,955 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
94 Citations
13,410 Views
18 Pages

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

  • Luca Éva Uhljar,
  • Sheng Yuan Kan,
  • Norbert Radacsi,
  • Vasileios Koutsos,
  • Piroska Szabó-Révész and
  • Rita Ambrus

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nan...

  • Article
  • Open Access
12 Citations
2,973 Views
10 Pages

Cancer, which is a leading cause of death, contributes significantly to reducing life expectancy worldwide. Even though paclitaxel (PTX) is known as one of the main anticancer drugs, it has several limitations, including low solubility in aqueous sol...

  • Article
  • Open Access
59 Citations
4,893 Views
14 Pages

Orodispersible Membranes from a Modified Coaxial Electrospinning for Fast Dissolution of Diclofenac Sodium

  • Tingbao Ning,
  • Yangjian Zhou,
  • Haixia Xu,
  • Shiri Guo,
  • Ke Wang and
  • Deng-Guang Yu

21 October 2021

The dissolution of poorly water-soluble drugs has been a longstanding and important issue in pharmaceutics during the past several decades. Nanotechnologies and their products have been broadly investigated for providing novel strategies for resolvin...

  • Article
  • Open Access
17 Citations
8,213 Views
15 Pages

Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR

  • Francesco Tres,
  • Steven R. Coombes,
  • Andrew R. Phillips,
  • Leslie P. Hughes,
  • Stephen A. C. Wren,
  • Jonathan W. Aylott and
  • Jonathan C. Burley

10 September 2015

We have investigated the dissolution performance of amorphous solid dispersions of poorly water-soluble bicalutamide in a Kollidon VA64 polymeric matrix as a function of the drug loading (5% vs. 30% bicalutamide). A combined suite of state-of-the-art...

  • Article
  • Open Access
18 Citations
4,502 Views
16 Pages

Formulation Development of Mirtazapine Liquisolid Compacts: Optimization Using Central Composite Design

  • Faiza Naureen,
  • Yasar Shah,
  • Sayyed Ibrahim Shah,
  • Muhammad Abbas,
  • Inayat Ur Rehman,
  • Salar Muhammad,
  • Hamdullah Hamdullah,
  • Khang Wen Goh,
  • Fazli Khuda and
  • Long Chiau Ming
  • + 3 authors

22 June 2022

Mirtazapine is a tetracyclic anti-depressant with poor water solubility. The aim of this study was to improve the dissolution rate of mirtazapine by delivering the drug as a liquisolid compact. Central composite design (CCD) was employed for the prep...

  • Article
  • Open Access
11 Citations
3,291 Views
18 Pages

Electro-Hydrodynamic Drop-on-Demand Printing of Aqueous Suspensions of Drug Nanoparticles

  • Ezinwa Elele,
  • Yueyang Shen,
  • Rajyalakshmi Boppana,
  • Afolawemi Afolabi,
  • Ecevit Bilgili and
  • Boris Khusid

We demonstrate the ability to fabricate dosage forms of a poorly water-soluble drug by using wet stirred media milling of a drug powder to produce an aqueous suspension of nanoparticles and then print it onto a porous biocompatible film. Contrary to...

  • Article
  • Open Access
12 Citations
5,193 Views
22 Pages

Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administrati...

  • Review
  • Open Access
197 Citations
16,566 Views
12 Pages

Hydrogel-Based Drug Delivery Systems for Poorly Water-Soluble Drugs

  • Matthew McKenzie,
  • David Betts,
  • Amy Suh,
  • Kathryn Bui,
  • London Doyoung Kim and
  • Hyunah Cho

13 November 2015

Hydrogels are three-dimensional materials that can withstand a great amount of water incorporation while maintaining integrity. This allows hydrogels to be very unique biomedical materials, especially for drug delivery. Much effort has been made to i...

  • Article
  • Open Access
813 Views
22 Pages

Impact of Different Surfactants on Oral Bioavailability of Paclitaxel/HPMC-AS Amorphous Solid Dispersion

  • Chenzhao Zhang,
  • Siyi Mao,
  • Jinhua Yuan,
  • Xiuzhen Ma,
  • Aiya Xing,
  • Xiaoling Liu and
  • Yuejie Chen

Objectives: Surfactants are commonly incorporated into amorphous solid dispersions (ASDs) to improve manufacturing and enhance the dissolution of poorly water-soluble drugs. However, their impact on in vitro dissolution, in vivo bioavailability, and...

  • Article
  • Open Access
71 Citations
7,167 Views
13 Pages

22 August 2022

The purpose of this study was to investigate the efficacy of hydrophilic polymers in a solid dispersion formulation in improving the solubility and dissolution rate of rivaroxaban (RXB), a poorly soluble drug. The developed solid dispersion consisted...

  • Article
  • Open Access
40 Citations
6,997 Views
11 Pages

Effect of Cyclodextrin Types and Co-Solvent on Solubility of a Poorly Water Soluble Drug

  • Suporn Charumanee,
  • Siriporn Okonogi,
  • Jakkapan Sirithunyalug,
  • Peter Wolschann and
  • Helmut Viernstein

18 October 2016

The aim of the study was to investigate the solubility of piroxicam (Prx) depending on the inclusion complexation with various cyclodextrins (CDs) and on ethanol as a co-solvent. The phase-solubility method was applied to determine drug solubility in...

  • Article
  • Open Access
52 Citations
3,744 Views
17 Pages

1 September 2024

Core–shell nanostructures are powerful platforms for the development of novel nanoscale drug delivery systems with sustained drug release profiles. Coaxial electrospinning is facile and convenient for creating medicated core–shell nanostructures with...

  • Article
  • Open Access
165 Citations
6,458 Views
16 Pages

Energy-Saving Electrospinning with a Concentric Teflon-Core Rod Spinneret to Create Medicated Nanofibers

  • Shixiong Kang,
  • Shicong Hou,
  • Xunwei Chen,
  • Deng-Guang Yu,
  • Lin Wang,
  • Xiaoyan Li and
  • Gareth R. Williams

20 October 2020

Although electrospun nanofibers are expanding their potential commercial applications in various fields, the issue of energy savings, which are important for cost reduction and technological feasibility, has received little attention to date. In this...

  • Article
  • Open Access
2 Citations
1,702 Views
14 Pages

Drug–Phospholipid Co-Amorphous Formulations: The Role of Preparation Methods and Phospholipid Selection

  • Keyoomars Khorami,
  • Sam Darestani Farahani,
  • Anette Müllertz and
  • Thomas Rades

Background/Objectives: This study aims to broaden the knowledge on co-amorphous phospholipid systems (CAPSs) by exploring the formation of CAPSs with a broader range of poorly water-soluble drugs, celecoxib (CCX), furosemide (FUR), nilotinib (NIL), a...

  • Article
  • Open Access
48 Citations
9,190 Views
15 Pages

13 August 2015

The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery sy...

  • Review
  • Open Access
296 Citations
20,522 Views
26 Pages

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic ant...

  • Review
  • Open Access
33 Citations
6,864 Views
19 Pages

Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs

  • Arvind Sharma,
  • Kanika Arora,
  • Harapriya Mohapatra,
  • Rakesh K. Sindhu,
  • Madalin Bulzan,
  • Simona Cavalu,
  • Gulsheen Paneshar,
  • Hosam O. Elansary,
  • Ahmed M. El-Sabrout and
  • Abdullah Alaklabi
  • + 1 author

At present, the majority of APIs synthesized today remain challenging tasks for formulation development. Many technologies are being utilized or explored for enhancing solubility, such as chemical modification, novel drug delivery systems (microemuls...

  • Review
  • Open Access
80 Citations
7,751 Views
21 Pages

Recent Technologies for Amorphization of Poorly Water-Soluble Drugs

  • Dohyun Kim,
  • Youngwoo Kim,
  • Yee-Yee Tin,
  • Mya-Thet-Paing Soe,
  • Byounghyen Ko,
  • Sunjae Park and
  • Jaehwi Lee

Amorphization technology has been the subject of continuous attention in the pharmaceutical industry, as a means to enhance the solubility of poorly water-soluble drugs. Being in a high energy state, amorphous formulations generally display significa...

  • Review
  • Open Access
195 Citations
17,312 Views
74 Pages

Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aque...

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