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Drug Development and Industrial Pharmacy

Kasturi R Pawar, Diane Render, Vijaya K Rangari, Yoon Y Lee, R Jayachandra Babu
OBJECTIVE: The objective of this study was to evaluate non-crystalline cellulose (NCC) as a novel tablet excipient in solid oral dosage forms in comparison with microcrystalline cellulose (MCC) and silicified microcrystalline cellulose (Prosolv®, SMCC). SIGNIFICANCE: MCC, although a widely used tablet excipient, has diasdvantages in terms of its low dilution potential for potent drugs, and sensitivity to lubricant and moisture. SMCC, a modified version of MCC, has improved tablet compression properties...
May 8, 2018: Drug Development and Industrial Pharmacy
Bader B Alsulays, Mohamed H Fayed, Ahmed Alalaiwe, Saad M Alshahrani, Abdullah S Alshetaili, Sultan M Alshehri, Fars K Alanazi
The objective of this study was to examine the influence of drug amount and mixing time on the homogeneity and content uniformity of a low-dose drug formulation during the dry mixing step using a new gentle-wing high shear mixer. Moreover, the study investigated the influence of drug incorporation mode on the content uniformity of tablets manufactured by different methods. Albuterol sulphate was selected as a model drug and was blended with the other excipients at two different levels, 1% w/w and 5% w/w at impeller speed of 300 rpm and chopper speed of 3000 rpm up to 30 minutes...
May 2, 2018: Drug Development and Industrial Pharmacy
Yingying Ding, Changyuan Wang, Yutong Wang, Youwei Xu, Jing Zhao, Meng Gao, Yanfang Ding, Jinyong Peng, Lei Li
BACKGROUND: Although piperine can inhibit cells of tumors, the poor water solubility restricted its clinical application. This paper aimed to develop mixed micelles based on Soluplus® and TPGS, to improve the aqueous solubility and anti-cancer effect. METHODS: Piperine -loaded mixed micelles were prepared using a thin- film hydration method, and their physicochemical properties were characterized. The cellular uptake of the micelles was confirmed by confocal laser scanning microscopy in A549 lung cancer cells and HepG2 liver cancer cells...
May 2, 2018: Drug Development and Industrial Pharmacy
Daniel Blackwood, William Ketterhagen, John Kresevic, Joseph Kushner, Jeffrey Moriarty, Matthew P Mullarney
The purpose of this work was to develop a methodology that quantifies the extent of shear induced during an encapsulation process and show how formulation composition and manufacturing process designs can be changed to reduce the negative impact on drug product quality attributes. The powder feed system used in a dosing disk type pharmaceutical capsule filling machine induced additional shear of the powder prior to slug formation. The shear occurred both in the hopper portion, via the rotation of the feed auger and impeller, and in the powder bowl via the tamping pin agitation and/or shear against the stationary surfaces such as the powder level scraper...
May 1, 2018: Drug Development and Industrial Pharmacy
Washington X De Paula, Ângelo M L Denadai, Aline N G Braga, Prasad Shastri, Sérgio V B Pinheiro, Frederic Frezard, Robson A S Santos, Rubén D Sinisterra
Losartan, a nonpeptidic orally active agent, reduces arterial pressure through specific and selective blockade of angiotensin II receptor AT1. However, this widely used AT1 antagonist presents low bioavailability and needs once or twice a day dosage. In order to improve its bioavailability, we used the host:guest strategy based on β-cyclodextrin (βCD). The results suggest that Losartan included in βCD showed a typical pulsatile release pattern after oral administration to rats, with increase of plasma levels of Losartan...
April 23, 2018: Drug Development and Industrial Pharmacy
Chun-Hui Zhai, Jian-Bang Xuan, Hai-Liu Fan, Teng-Fei Zhao, Jian-Lan Jiang
In order to make a further optimization of process design via increasing the stability of design space, we brought in the model of Support Vector Regression (SVR). In this work, the extraction of podophyllotoxin was researched as a case study based on QbD. We compared the fitting effect of SVR and the most used quadratic polynomial model (QPM) in QbD, and an analysis was made between the two design spaces obtained by SVR and QPM. As a result, the SVR stayed ahead of QPM in prediction accuracy, the stability of model and the generalization ability...
April 20, 2018: Drug Development and Industrial Pharmacy
Rania Hamed, Ala'a AbuRezeq, Ola Tarawneh
Periodontal disease is a chronic inflammation of gum and tissues that surround and support the teeth. Nonsteroidal anti-inflammatory drugs (NSAIDs) can be used in the treatment of periodontitis to ease swelling and inflammation. One approach of treating periodontitis is loading the NSAIDs in local drug delivery systems. Therefore, the objective of this study was to investigate the local delivery of the NSAIDs model drug ibuprofen to treat periodontitis using different types of gel formulations (hydrogel, oleogel, and bigel)...
April 19, 2018: Drug Development and Industrial Pharmacy
Shahinaze A Fouad, Rehab N Shamma, Emad B Basalious, Mohamed M El-Nabarawi, Saadi A Tayel
Dapoxetine (D) suffers from poor oral bioavailability (42%) due to extensive metabolism in the liver. The aim of this study was to enhance the bioavailability of D via preparing instantly-dispersible nanocarrier powder system (IDNPs) for intranasal delivery of D. IDNPs were prepared using the thin film hydration technique, followed by freeze-drying to obtain easily reconstituted powder providing rapid and ready method of administration. The produced nanocarrier systems were evaluated for drug content, entrapment efficiency percentage, particle size, polydispersity index, zeta potential, and drug payload...
April 18, 2018: Drug Development and Industrial Pharmacy
Xu Liu, Mingshuang Li, Hugh Smyth, Feng Zhang
Disorders of the ear severely impact the quality of life of millions of people, but the treatment of these disorders is an on-going but often overlooked challenge particularly in terms of formulation design and product development. The prevalence of ear disorders has spurred significant efforts to develop new therapeutic agents, but perhaps less innovation has been applied to new drug delivery systems to improve the efficacy of ear disease treatments. This review provides a brief overview of physiology, major diseases, and current therapies used via the otic route of administration...
April 16, 2018: Drug Development and Industrial Pharmacy
Peter Dogterom, ChauHwei Fu, Thomas Legg, Yi-Jin Chiou, Steve Brandon
OBJECTIVE: To assess absolute bioavailability of 20 mEq Magnesium lactate extended release (ER) caplets and to assess the effect of food on the pharmacokinetics of these ER caplets. SIGNIFICANCE: Magnesium in different salt forms is available as over-the-counter oral formulations. The absorption and bioavailability is highly affected by water solubility of the salt form. A new ER caplet of 10 mEq strength of Magnesium L-lactate dihydrate has been developed to increase bioavailability of magnesium...
April 11, 2018: Drug Development and Industrial Pharmacy
Boshra Amiri, Hasan Ahmadvand, Ali Farhadi, Aazam Najmafshar, Mohsen Chiani, Dariush Norouzian
Vinblastine (VB), as a chemotherapeutic agent, is widely used in treatment of different types of cancer. However, its clinical application is limited due to its low water solubility, side effects, and multidrug resistance. The aim of this study was to increase the therapeutic efficacy of VB using drug delivery systems. For this purpose, a PEGylated niosomal formulation of vinblastine (Pn-VB) was prepared by thin film hydration method and physicochemically characterized. Drug release pattern was performed by dialysis diffusion method...
April 11, 2018: Drug Development and Industrial Pharmacy
Baixue Yang, Chen Wei, Yang Yang, Qifang Wang, Sanming Li
OBJECTIVE: To evaluate parameters about wettability, water absorption or swelling of excipients in forms of powders or dosage through various methods systematically and explore its correlation with tablet disintegration. MATERIAL AND METHODS: The water penetration and swelling of powders with different proportions of excipients including microcrystalline cellulose (MCC), mannitol, low-substituted hydroxypropyl cellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), croscarmellose sodium (CCMC-Na) and magnesium stearate (MgSt) were determined by Washburn capillary rise...
April 6, 2018: Drug Development and Industrial Pharmacy
Dharmesh Gol, Shreya Thakkar, Manju Misra
OBJECTIVE: In present work nanocrystal based formulation of Risperidone (RIS) was proposed to overcome solubility issue of RIS, while lyophilization technique was used effectively, for conversion of RIS nanosuspension to solid state. SIGNIFICANCE: RIS nanosuspension was developed and stabilized with a combination of Polycaprolactone and Pluronic® F-68 as stabilizers. With focus on critical parameters like nature of cryoprotectants and effect of eutectic temperature on properties of nanosuspension, the suitability of lyophilization technique in improving the physical stability of prepared nanosuspension was also evaluated...
April 5, 2018: Drug Development and Industrial Pharmacy
Leah Wright, Shasha Rao, Nicky Thomas, Ramiz A Boulos, Clive A Prestidge
OBJECTIVE: Novel antibiotic Ramizol® is advancing to clinical trials for the treatment of gastrointestinal Clostridium difficile associated disease. Despite this, previous studies have shown a rapid plasma clearance upon intravenous administration and low oral bioavailability indicating pure drug is unsuitable for systemic infection treatment following oral dosing. The current study aims to investigate the development of poly-lactic-(co-glycolic) acid (PLGA) particles to overcome this limitation and increase the systemic half-life following subcutaneous and intramuscular dosing...
April 5, 2018: Drug Development and Industrial Pharmacy
Zahra Daman, Homa Faghihi, Hamed Montazeri
Recently, Salinomycin (SAL) has been reported to inhibit proliferation and induce apoptosis in various tumors. The aim of this study was to deliver SAL to orthotopic model of pancreatic cancer by the aid of poly (lactic-co-glycolic acid) (PLGA) nanoparticles. The nanoparticles were physico-chemically characterized and evaluated for cytotoxicity on Luciferase-transduced AsPC-1 cells in vitro as well as implanted orthotopically into the pancreas of nude mice. SAL (3.5 mg/kg every other day) blocked tumor growth by 52% compared to the control group after 3 weeks of therapy...
April 5, 2018: Drug Development and Industrial Pharmacy
Ariane J Sousa-Batista, Natalia Arruda-Costa, Bartira Rossi-Bergmann, Maria Inês Ré
Current chemotherapy of cutaneous leishmaniasis (CL), even the mildest forms, encompasses multiple and painful injections with toxic drugs that cause systemic adverse effects. Recently, we showed the promising use of PLGA microparticles loaded with an antileishmanial nitrosylated chalcone (CH8) for effective, safe, local and single-dose treatment of CL. Here, we proposed to optimize the delivery system by increasing the CH8 loading in PLGA-microparticles using spray drying instead of emulsification-solvent evaporation...
April 5, 2018: Drug Development and Industrial Pharmacy
Jun-Yong Wu, Yong-Jiang Li, Meng Han, Xiong-Bin Hu, Le Yang, Jie-Min Wang, Da-Xiong Xiang
Puerarin is a phytochemical with various pharmacological effects, but poor water solubility and low oral bioavailability limited usage of puerarin. The purpose of this study was to develop a new microemulsion (ME) based on phospholipid complex technique to improve the oral bioavailability of puerarin. Puerarin phospholipid complex (PPC) was prepared by a solvent evaporation method and was characterized by X-ray diffraction and infrared spectroscopy. Pseudo-ternary phase diagrams were constructed to investigate the effects of different oil on the emulsifying performance of the blank ME...
April 5, 2018: Drug Development and Industrial Pharmacy
Sarah Baltzley, Azzam A Malkawi, Motasem Alsmadi, Abeer M Al-Ghananeem
INTRODUCTION: The aim of this study was to investigate Ketorolac (KT) systemic absolute bioavailability after sublingual (SL) administration in vivo to conscious rabbits. Furthermore, the study investigated the potential use of chitosan nanoparticles as a delivery system to enhance the systemic bioavailability of KT following sublingual administration. METHODS: Ketorolac-loaded chitosan nanoparticles were prepared through ionotropic gelation of chitosan with tripolyphosphate anions...
April 2, 2018: Drug Development and Industrial Pharmacy
Sarunya Tuntiyasawasdikul, Ekapol Limpongsa, Napaphak Jaipakdee, Bungorn Sripanidkulchai
RATIONAL: Phytoestrogens have been found to delay signs of skin aging in post-menopausal women, in a way similar to the effects of estrogens. Diarylheptanoids from a rhizome of traditional Thai herb named Curcuma comosa is considered to be a novel class of phytoestrogens. OBJECTIVES: The aims of this study were to prepare effective topical films using mixed types and vary ratios of hydrophobic (Eudragit RL, Eudragit RS, and Eudragit NE) and hydrophilic polymer (hydroxylpropyl methycellulose, HPMC) with Transcutol as a permeation enhancer for delivery of diarylheptanoids to improve signs of skin aging in post-menopausal women...
March 26, 2018: Drug Development and Industrial Pharmacy
Hamed Nosrati, Maral Adibtabar, Ali Sharafi, Hossein Danafar, Manjili Hamidreza Kheiri
Denderimer-modified magnetic nanoparticles are a promising drug delivery nanosystem which can improve the therapeutic efficacy of chemotherapy drugs and can also be beneficial as magnetic resonance (MR) images contrast agent. The present study introduces the preparation and characterization of the potential therapeutic efficiency of curcumin (CUR)-loaded denderimer-modified citric acid coated Fe3 O4 NPs. Polyamidoamine (PAMAM, generation G5 ) was used to encapsulate citric acid coated Fe3 O4 nanoparticles. The successful preparation of CUR-loaded nanocarriers were confirmed by X-ray diffraction (XRD), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), vibrating sample magnetometer (VSM), and transmission electron microscopy (TEM) techniques...
March 23, 2018: Drug Development and Industrial Pharmacy
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