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Drug Development and Industrial Pharmacy

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https://www.readbyqxmd.com/read/30411991/enhancing-oral-bioavailability-of-poorly-soluble-drugs-with-mesoporous-silica-based-systems-opportunities-and-challenges
#1
Kristen E Bremmell, Clive A Prestidge
Porous silica based drug delivery systems have shown considerable promise for improving the oral delivery of poorly water-soluble drugs. More specifically, micro- and meso-porous silica carriers have high surface areas with associated ability to physically adsorb high drug loads in a molecular or amorphous form; this allows molecular state drug release in aqueous gastro-intestinal environments, potential for supersaturation, and hence facilitates enhanced absorption and increased bioavailability. This review focuses primarily on the ability of porous silica materials to modulate in vitro drug release and enhance in vivo biopharmaceutical performance...
November 9, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30404554/nanoencapsulation-of-betamethasone-valerate-using-high-pressure-homogenization-solvent-evaporation-technique-optimisation-of-formulation-and-process-parameters-for-efficient-dermal-targeting
#2
Shadab Md, Jasvinder Kaur A/P Kuldeep Singh, Muhammad Waqas, Manisha Pandey, Hira Choudhury, Haroon Habib, Fahad Hussain, Zahid Hussain
Betamethsone valerate (BMV), a medium potency topical corticosteroid, is one of the most commonly employed pharmacological agents for the management of atopic dermatitis (AD) in both adults and children. Despite having remarkable pharmacological efficacy, these agents have limited clinical implication due to poor penetration across the startum cornum (SC). To mitigate issues related to targeted delivery, stability, and solubility as well as to potentiate therapeutic and clinical implication, the nanodelivery systems have gained remarkable recognition...
November 8, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30395728/oral-delivery-of-the-anti-tnf%C3%AE-domain-antibody-v565-results-in-high-intestinal-and-faecal-concentrations-with-minimal-systemic-exposure-in-cynomolgus-monkeys
#3
J Scott Crowe, Kevin J Roberts, Timothy M Carlton, Luana Maggiore, Marion F Cubitt, Keith P Ray, Mary C Donnelly, John C Wahlich, Jonathan I Humphreys, Jan R Robinson, Gary A Whale, Michael R West
OBJECTIVE: V565 is a novel oral anti-TNFα domain antibody being developed for topical treatment of inflammatory bowel disease (IBD) patients. Protein engineering rendered the molecule resistant to intestinal proteases. Here we investigate the formulation of V565 required to provide gastro-protection and enable optimal delivery to the lower intestinal tract in monkeys. METHODS: Enteric coated V565 mini-tablets were prepared and dissolution characteristics tested in vitro...
November 5, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30395722/a-comparison-of-drug-substance-predicted-chemical-stability-with-ich-compliant-stability-studies
#4
H E Williams, J Bright, E Roddy, A Poulton, S D Cosgrove, F Turner, P Harrison, A Brookes, E MacDougall, A Abbott, C Gordon
Objective - The aim of this study is to demonstrate the applicability of predictive stability studies to the degradation of drug substances. Significance - The use of predicted stability studies during pharmaceutical development and in regulatory submissions is increasing, particularly in early phase to support an initial retest period/shelf life claim in the absence of standard stability data. These studies offer an alternative to standard stability testing and can facilitate clinical trials to be started earlier and medicines to reach patients faster...
November 5, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30394795/formulation-optimization-heamocompatibility-and-pharmacokinetic-evaluation-of-plga-nanoparticles-containing-paclitaxel
#5
Pooja Mittal, Harsh Vardhan, Gufran Ajmal, Gunjan Vasant Bonde, Ramit Kapoor, Ashu Mittal, Brahmeshwar Mishra
OBJECTIVE: Paclitaxel (PTX) loaded Polymer (PLGA) based nanoformulation was developed with the objective of formulating cremophore EL free nanoformulation intended for i.v use. SIGNIFICANCE: The polymeric PTX nanoparticles free from the cremophore EL will help in eliminating the shortcomings of the existing delivery system as cremophore EL causes serious allergic reactions to the subjects after intravenous use. Methods& Results: PTX loaded nanoparticles were formulated by nanoprecipitation method...
November 5, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30388376/nanodispersions-stabilized-by-%C3%AE-cyclodextrin-nanosponges-application-for-simultaneous-enhancement-of-bioactivity-and-stability-of-sage-essential-oil
#6
Yacine Nait Bachir, Ryma Nait Bachir, Amel Hadj-Ziane-Zafour
The aim of the present work was to stabilize oil-in-water nanoemulsion containing sage (salvia officinalis) essential oil, for enhancing its physicochemical stability and enlarging its industrial applications. New β-cyclodextrin nanosponges were synthesized by polycondensation using naphthalene dicarboxylic acid as cross-linking agent, the latter system was characterized by FTIR spectroscopy, SEM, BET and powder XRD. Nanoemulsions stabilized by free β-cyclodextrin or nanosponges were prepared, their physicochemical properties were determined (particles size, zeta potential, viscosity, turbidity and essential oil content) and their stability was studied at different storage temperatures (4 °C, 20 °C and 40 °C) during 3 months...
November 2, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30231652/assessment-of-lisdexamfetamine-dimesylate-stability-and-identification-of-its-degradation-product-by-nmr-spectroscopy
#7
Graciela Carlos, Alvicler Magalhães, Ana Cristina Isler, Eloisa Comiran, Pedro Eduardo Fröehlich
Lisdexamfetamine dimesylate (LDX), a long-acting prodrug stimulant indicated for the treatment of the attention-deficit/hyperactivity disorder (ADHD), was subjected to forced degradation studies by acid and alkaline hydrolysis and the degradation profile was studied. To obtain between 10-30% of degraded product, acid and alkaline conditions were assessed with solutions of 0.01 M, 0.1 M, 0.5 M, and 1 M of DCl and NaOD. These solutions were analyzed through 1 H NMR spectra. Acid hydrolysis produced no degradation in 0...
November 1, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30303407/tolmetin-sodium-loaded-thermosensitive-mucoadhesive-liquid-suppositories-for-rectal-delivery-strategy-to-overcome-oral-delivery-drawbacks
#8
Mohamed A Akl, Hatem R Ismael, Fathy I Abd Allah, Alla A Kassem, Ahmed M Samy
Tolmetin sodium (TS) is a nonsteroidal anti-inflammatory drug (NSAID) indicated for treatment of musculoskeletal issues. As other NSAID, TS displays a marked side effects on the gastro-intestinal (GI) tract after oral administration. Traditional solid suppositories can cause pain and discomfort for patients, may reach the end of the colon; consequently, the drug can undergo the first-pass effect. TS liquid suppository (TS-LS ) was developed to enhance patient compliance and rectal mucosal safety in high-risk patients receiving highly NSAID therapy...
October 31, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30372644/influencing-factors-on-gelatin-matrix-for-chlorhexidine-delivery
#9
Michael Murawsky, Gary R Kelm, Darby Kozak, Bin Qin, Yuan Zou, S Kevin Li
OBJECTIVE: The objective was to evaluate the influencing factors in the fabrication of gelatin matrix (gelatin chips) for drug delivery. The attributes affecting drug release characteristics of the gelatin products were examined. SIGNIFICANCE: Understanding the attributes that affect drug release from gelatin matrix could provide the knowledge base for the development, manufacturing, and performance evaluation of gelatin based drug products for sustained drug delivery...
October 29, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30366501/efficient-method-for-isolation-of-exosomes-from-raw-bovine-milk
#10
Marika Yamauchi, Kaori Shimizu, Md Matiur Rahman, Hinata Ishikawa, Hiroshi Takase, Shinya Ugawa, Ayaka Okada, Yasuo Inoshima
OBJECTIVE: This study aimed to establish a rapid and simple method for isolating exosomes from raw bovine milk and to compare the quality of the isolated exosomes with those isolated by a standard method involving ultracentrifugation (UC). METHODS: To remove caseins, which are major milk proteins consisting more than 80% of milk protein (35% in human breast milk) and hamper isolation and purification of exosomes, hydrochloride (HCl) was added to milk for isoelectric precipitation (IP)...
October 26, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30307339/simultaneous-determination-of-methocarbamol-and-aspirin-in-presence-of-their-pharmacopeial-related-substances-in-combined-tablets-using-novel-hplc-dad-method
#11
Fawzi A El-Yazbi, Omayma A Amin, Eman I El-Kimary, Essam F Khamis, Sameh E Younis
Objective and Significance: Methocarbamol (MET) and aspirin (ASP) are widely used as a muscle relaxant combination. The USP reports guaifenesin (GUA) and salicylic acid (SAL) as related substances and hydrolytic products of MET and ASP, respectively. This work aimed at developing and validating a simple and sensitive RP-HPLC method for the determination of both drugs as well as their related substances (at their pharmacopeial limits) in their bulk powders, laboratory prepared mixtures, and MET-ASP combined tablets...
October 26, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30229685/mechanism-of-enhanced-oral-absorption-of-akebia-saponin-d-by-a-self-nanoemulsifying-drug-delivery-system-loaded-with-phospholipid-complex
#12
Yuhui Wang, Jinyang Shen, Xiaolin Yang, Ye Jin, Zhonglin Yang, Rufeng Wang, Fuming Zhang, Robert J Linhardt
Akebia saponin D (ASD) exhibits a variety of pharmacological activities, such as anti-osteoporosis, neuroprotection, hepatoprotection, but has poor oral bioavailability. A self-nanoemulsifying drug delivery system loaded with akebia saponin D - phospholipid complex (APC-SNEDDS) (composition: Peceol: Cremophor® EL: Transcutol HP: ASD: phospholipid; ratio: 10:45:45:51:12.3, w:w:w:w:w) was first developed to improve the oral absorption of saponins and it was found to significantly enhance ASD's oral bioavailability by 4...
October 26, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30231654/research-on-the-relationship-between-cephalosporin-structure-solution-clarity-and-rubber-closure-compatibility-using-volatile-components-profile-of-butyl-rubber-closures
#13
Xiao-Meng Chong, Xin Dong, Shang-Chen Yao, Chang-Qin Hu
OBJECTIVE: Establish an effective experimental strategy to determine the compatibility of rubber closures for drugs. SIGNIFICANCE: Various types of rubber closures with different compositions are available for drug packaging. Many additives of rubber closures can be released from rubber closures and may affect the quality of drugs and pose a risk to human health. In this study, we aimed to determine the relationship between cephalosporin structure, solution clarity, and rubber closure compatibility using volatile components profile of butyl rubber closures...
October 24, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30231647/influence-of-punch-geometry-head-flat-diameter-and-tooling-type-b-or-d-on-the-physical-mechanical-properties-of-formulation-tablets
#14
Harsh G Shah, Rohit P Dugar, HongHao Li, Vivek S Dave, Rutesh H Dave
The presented study assessed the influence of punch geometry (head-flat [HF] diameter) and tooling type ('B' or 'D') on the physical-mechanical properties of tablets prepared by direct-compression of two guaifenesin (25% or 40% w/w) formulations. Tablets of both formulations were prepared on instrumented, single-layer, rotary tablet press using 10 mm, flat-faced, 'B' or 'D'-type tooling with different HF diameters, and compression forces (CF) ranging from 5 to 25 kN with 5 kN increments. The tablets were evaluated for dimensions, weight variation, tensile strength (TS), friability, and capping index...
October 24, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30230386/brain-targeting-of-chitosan-based-diazepam-mucoadhesive-microemulsions-via-nasal-route-formulation-optimization-characterization-pharmacokinetic-and-pharmacodynamic-evaluation
#15
Srividya Ramreddy, Krishnaveni Janapareddi
OBJECTIVE: The aim of present investigation was to develop microemulsions (MEs) and mucoadhesive microemulsions (MME) of diazepam for brain uptake through nasal administration for the treatment of seizure emergency. SIGNIFICANCE: Status epilepticus (SE) is a medical emergency, requires intravenous administration of diazepam which requires hospitalization of patient. Initiation of therapy at home via nasal administration of diazepam could prevent the damage of brain due to delay of therapy initiation...
October 24, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30348020/formulation-optimization-of-solid-lipid-nanocarrier-system-of-stat3-inhibitor-to-improve-its-activity-in-triple-negative-breast-cancer-cells
#16
Sai Kiran S S Pindiprolu, Pavan Kumar Chintamaneni, Praveen T Krishnamurthy, Kinnera Ratna Sree Ganapathineedi
In the present study, solid lipid nanoparticles (SLNs) have been formulated as a carrier system for effective intracellular delivery of STAT3 inhibitor, niclosamide (Niclo) to triple negative breast cancer (TNBC) cells. Emulsification-solvent evaporation method was employed in formulation of Niclo loaded SLNs (Niclo-SLNs). The formula of Niclo-SLN was optimized by Box-Behnken design and characterized for their shape, size and surface charge. The in vitro anti-cancer efficacy of Niclo-SLNs was studied in TNBC cells...
October 23, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30348012/the-effect-of-ferrous-ions-calcium-ions-and-citric-acid-on-absorption-of-ciprofloxacin-across-caco-2-cells-practical-and-structural-approach
#17
Dina El-Sabawi, Rana Abu-Dahab, Waleed A Zalloum, Fadia Ijbara, Imad I Hamdan
OBJECTIVE: To study the potential influence of selected metal ions on absorption (and hence oral bioavailability of ciprofloxacin (Cipro) in presence and absence of a competing ligand. SIGNIFICANCE: The presence of metal ions together with Cipro results in complexes exhibiting a decreased bioavailability. Attempts were made to better understand the mechanism of decreased Cipro bioavailability in the presence of metals such as calcium and ferrous ions, and a small-sized ligand citric acid (CitA)...
October 23, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30348022/microneedles-for-transdermal-drug-delivery-a-systematic-review
#18
Saili Dharadhar, Anuradha Majumdar, Sagar Dhoble, Vandana Patravale
Transdermal route has been explored for various agents due to its advantage of by passing the first pass effect and sustained release of drug. Due to strong barrier properties of the skin, mainly stratum corneum (SC), the delivery of many therapeutic agents across the skin has become challenging. Few drugs with specific physicochemical properties (molecular weight < 500 Da, adequate lipophilicity and low melting point) can be effectively administered via transdermal route. However, delivery of hydrophilic drugs and macromolecular agents including peptides, DNA and small interfering RNA is challenging...
October 22, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30346852/development-and-evaluation-of-hollow-mesoporous-silica-microspheres-bearing-on-enhanced-oral-delivery-of-curcumin
#19
Yang Gao, Shujiang Ding, Xiaoyan Huang, Zhaoyang Fan, Jianmei Sun, Yang Hai, Kai Li
The aim of this work is to develop curcumin-loaded hollow mesoporous silica microspheres (HMSMs@curcumin) to improve the poor oral bioavailability of curcumin. Hollow mesoporous silica microspheres (HMSMs) were synthesized in facile route using a hard template. HMSMs and HMSMs@curcumin were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption/desorption measurements, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) and X-ray diffraction (XRD)...
October 22, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/30346842/a-w-o-emulsion-mediated-film-dispersion-method-for-curcumin-encapsulated-ph-sensitive-liposomes-in-the-colon-tumor-treatment
#20
Yi Chen, Qianming Du, Qianqian Guo, Jing Huang, Lina Liu, Xiangchun Shen, Jianqing Peng
The CaCO3 encapsulated liposome with pH sensitivity is an efficient carrier for the delivery of chemotherapeutic drugs. Herein, we provided an innovative method that take advantage of a W/O emulsion to prepare CaCO3 encapsulated liposomes for the delivery of curcumin. The liposomes with both CaCO3 and curcumin encapsulated (LCC) showed highly sensitivity to reduced pH (the environment of lysosomes). Due to the inherent pH sensitivity of CaCO3 , LCC swelled and released the encapsulated curcumin rapidly in acidic medium...
October 22, 2018: Drug Development and Industrial Pharmacy
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