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AAPS PharmSciTech

Marwa Ahmed Sallam, Ahmed O Elzoghby
Zein is a naturally occurring corn protein having similarity to skin keratin. Owing to its hydrophobicity and biodegradability, zein nanocarriers are promising drug delivery vehicles for hydrophobic dermatological drugs. In this study, zein-based nanocapsules (ZNCs) were exploited for the first time as dermal delivery carriers for flutamide (FLT), an antiandrogen used for the management of pilosebasceous unit disorders. FLT-loaded ZNC of appropriate particle size and negative surface charge were prepared by nanoprecipitation method...
June 7, 2018: AAPS PharmSciTech
Caroline Alvebratt, Ocean Cheung, Maria Strømme, Christel A S Bergström
Effective and compound-sparing methods to evaluate promising drug delivery systems are a prerequisite for successful selection of formulations in early development stages. The aim of the study was to develop a small-scale in situ method to determine drug release and supersaturation in highly concentrated suspensions of enabling formulations. Mesoporous magnesium carbonate (MMC), which delivers the drug in an amorphous form, was selected as a drug carrier. Five model compounds were loaded into the MMC at a 1:10 ratio using a solvent evaporation technique...
June 6, 2018: AAPS PharmSciTech
Filippos Kesisoglou, Maria Vertzoni, Christos Reppas
Physiologically based absorption modeling has been attracting increased attention to study the interactions of weakly basic drug compounds with acid-reducing agents like proton-pump inhibitors and H2 blockers. Recently, standardized gastric and intestinal biorelevant media to simulate the achlorhydric and hypochlorhydric stomach were proposed and solubility and dissolution data for two model compounds were generated. In the current manuscript, for the first time, we report the utility of these recently proposed biorelevant media as input into physiologically based absorption modeling...
June 5, 2018: AAPS PharmSciTech
Huner K Omer, Nozad R Hussein, Amina Ferraz, Mohammad Najlah, Waqar Ahmed, Kevin M G Taylor, Abdelbary M A Elhissi
Proliposome formulations containing salbutamol sulphate (SS) were developed using spray drying, and the effects of carrier type (lactose monohydrate (LMH) or mannitol) and lipid to carrier ratio were evaluated. The lipid phase comprised soy phosphatidylcholine (SPC) and cholesterol (1:1), and the ratios of lipid to carrier were 1:2, 1:4, 1:6, 1:8 or 1:10 w/w. X-ray powder diffraction (XRPD) revealed an interaction between the components of the proliposome particles, and scanning electron microscopy (SEM) showed that mannitol-based proliposomes were uniformly sized and spherical, whilst LMH-based proliposomes were irregular and relatively large...
June 5, 2018: AAPS PharmSciTech
Alice Melocchi, Federico Parietti, Simone Maccagnan, Marco Aldo Ortenzi, Stefano Antenucci, Francesco Briatico-Vangosa, Alessandra Maroni, Andrea Gazzaniga, Lucia Zema
Following recent advances in nutrigenomics and nutrigenetics, as well as in view of the increasing use of nutraceuticals in combination with drug treatments, considerable attention is being directed to the composition, bioefficacy, and release performance of dietary supplements. Moreover, the interest in the possibility of having such products tailored to meet specific needs is fast growing among costumers. To fulfill these emerging market trends, 3D-printed capsular devices originally intended for conveyance and administration of drugs were proposed for delivery of dietary supplements...
June 5, 2018: AAPS PharmSciTech
Monika Lavan, Gregory Knipp
The potential applications of dendrimer-like biopolymers (DLB) as stabilizing excipients for amorphous solid dispersion (ASD) of niclosamide, celecoxib, and resveratrol were evaluated based on (1) the formation and physical stability of the ASD and (2) the permeability and flux of the agents across Caco-2 cell monolayers. The evaluation was made by comparing the performance of prototype phytoglycogen derivatives (DLB1, DLB2, and DLB3) with commonly used polymers such as HPMCAS, PVPVA, and Soluplus®. PXRD was used to confirm the formation of the dispersions and detect crystallinity peaks formed during 2- and 4-week storage at 40°C/75% RH...
June 4, 2018: AAPS PharmSciTech
Jessica Silva, Maria Mendes, Tânia Cova, João Sousa, Alberto Pais, Carla Vitorino
Designing nanoparticle formulations with features tailored to their therapeutic targets in demanding timelines assumes increased importance. In this context, nanostructured lipid carriers (NLCs) offer an excellent example of a drug delivery nanosystem that has been broadly explored in the treatment of glioblastoma multiforme (GBM). Distinct fundamental NLC quality attributes can be harnessed to fit this purpose, namely particle size, size distribution, and zeta potential. These critical aspects intrinsically depend on the formulation components, influencing drug loading capacity, drug release, and stability of the NLCs...
June 4, 2018: AAPS PharmSciTech
Haichen Nie, Huaping Mo, Stephen R Byrn
Understanding physicochemical stability of darunavir ethanolate is expected to be of critical importance for the development and manufacturing of high-quality darunavir-related pharmaceutical products. However, there are no enabling monographs for darunavir to illustrate its solid-state chemistry, impurity profile, and assay methods. In addition, the US Pharmacopeia reference standard of darunavir is still not commercially available. It has been also challenging to find reliable vendors to obtain highly purified darunavir ethanolate crystals to conduct the physicochemical stability testing...
June 4, 2018: AAPS PharmSciTech
Gabriela Maria D'Angelo Costa, Claudinéia Aparecida Sales de Oliveira Pinto, Vânia Rodrigues Leite-Silva, André Rolim Baby, Maria Valéria Robles Velasco
Vitamin D3 supplementation is important to prevent and treat hypovitaminosis that is a worldwide public health issue. Most types of supplementation are by oral route or fortification foods. The alternative route must be investigated, as transdermal route, for people with fat malabsorption or other diseases that impair the absorption of vitamin D3 . This study focused on verifying the feasibleness of vitamin D3 skin retention and permeation with the presence of chemical penetration enhancers (soybean lecithin, isopropyl palmitate, propylene glycol, ethoxydiglycol, and cereal alcohol) at different pharmaceutical forms (gel and cream) through a human skin...
June 4, 2018: AAPS PharmSciTech
Daniel J Ellenberger, Dave A Miller, Sandra U Kucera, Robert O Williams
Ritonavir is an anti-viral compound that has also been employed extensively as a CYP3A4 and P-glycoprotein (Pgp) inhibitor to boost the pharmacokinetic performance of compounds that undergo first pass metabolism. For use in combination products, there is a desire to minimize the mass contribution of the ritonavir system to reduce patient pill burden in these combination products. In this study, KinetiSol® processing was utilized to produce an amorphous solid dispersion of ritonavir at two times the drug load of the commercially available form of ritonavir, and the composition was subsequently developed into a tablet dosage form...
June 4, 2018: AAPS PharmSciTech
Alaadin E El-Haddad, Nermin M Sheta, Sylvia A Boshra
The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2 -induced lung toxicity in rats. Morin was isolated from hydroalcoholic (70%) extract of Psidium guajava leaves by MPLC. The purity (> 90%) was done using HPLC. Screening of Morin solubility was studied to identify the components of each system...
June 4, 2018: AAPS PharmSciTech
Yu Xiao, Shuang Wang, Qingyu Zong, Zongning Yin
Single chemotherapeutic agent like paclitaxel (PTX) has shown some limitations in anti-tumor treatment, such as undesirable side effects, multidrug resistance, and high toxicity. In order to reduce the toxicity of PTX and increase the anti-tumor effect, folate-modified amphiphilic and biodegradable biomaterial was developed to co-deliver PTX and metformin (MET) for exerting the synergistic effect. PTX was physically entrapped in the hydrophobic inner core of the amphiphilic block copolymer by a solvent evaporation method, whereas MET was chemically conjugated to the hydrophilic terminals of copolymer via a pH-sensitive cis-aconityl linkage (Cis)...
June 4, 2018: AAPS PharmSciTech
Xingqi Wang, Yong Zhang, Shuangying Gui, Jie Huang, Jiaojiao Cao, Zhengguang Li, Qian Li, Xiaoqin Chu
Liquid crystals (LCs) are conventionally divided into thermotropic or lyotropic, based on the organization and sequence of the controlled molecular system. Lipid-based lyotropic liquid crystal (LLC), such as lamellar (Lα), bicontinuous cubic (QII ), or hexagonal (HII ) phases, have attracted wide interest in the last few decades due to their practical potential in diverse applications and notable structural complexity. Various guest molecules, such as biopharmaceuticals, chemicals, and additives, can be solubilized in either aqueous or oily phase...
June 4, 2018: AAPS PharmSciTech
Samia M Omar, Fathy I AbdAlla, Noha M Abdelgawad
Optimization of a lyophilized fast-disintegrating tablet (LFDT) formulation containing naratriptan hydrochloride, an antimigraine drug, was the foremost objective of the study, aiming in achieving fast headache pain relief. The Design-Expert® v10 software was used to generate formulations using D-optimal mixture design with four components: gelatin (X1 ), hydrolyzed gelatin (X2 ), glycine (X3 ), and mannitol (X4 ) of total solid material (TSM) w/w. The effect of the relative proportion of each component was determined on friability (Y1 ), hardness (Y2 ), and in vitro disintegration time (Y3 ), which was then applied for formulation optimization...
June 4, 2018: AAPS PharmSciTech
Hwahsiung P Lee, Yuriy Gulak, Alberto M Cuitino
Manufacturing of pharmaceutical tablets from powders is always accompanied by the conversion of irreversible mechanical work of compaction into heat. The heat is generated due to friction between powder particles, particles and the die wall, plastic deformation of particles, bonding, and other irreversible processes. The resulting temperature increase potentially might have significant effects on a tablet's mechanical properties, disintegration time, and drug release. In the present work, we show that using infrared thermography as a nondestructive and noncontact process analytical technology (PAT) tool to measure the tablet's rate of cooling, in contrast to the temperature evolution, can be directly related to the tablet's thermal diffusivity...
June 4, 2018: AAPS PharmSciTech
Monica R P Rao, Jagruti Chaudhari, Francesco Trotta, Fabrizio Caldera
Rilpivrine is BCS class II drug used for treatment of HIV infection. The drug has low aqueous solubility (0.0166 mg/ml) and dissolution rate leading to low bioavailability (32%). Aim of this work was to enhance solubility and dissolution of rilpivirine using beta-cyclodextrin-based nanosponges. These nanosponges are biocompatible nanoporous particles having high loading capacity to form supramolecular inclusion and non-inclusion complexes with hydrophilic and lipophilic drugs for solubility enhancement. Beta-cyclodextrin was crosslinked with carbonyl diimidazole and pyromellitic dianhydride to prepare nanosponges...
June 4, 2018: AAPS PharmSciTech
Jeffry D Schroeter, Poonam Sheth, Anthony J Hickey, Bahman Asgharian, Owen T Price, Jay T Holt, Denise S Conti, Bhawana Saluja
The performance of pressurized metered dose inhalers (MDIs) is affected by formulation and device variables that impact delivered dose, aerodynamic particle size distribution, and consequently lung deposition and therapeutic effect. Specific formulation variables of relevance to two commercially available products-Proventil® HFA [albuterol sulfate (AS) suspension] and Qvar® [beclomethasone dipropionate (BDP) solution]-were evaluated to determine their influence on key performance attributes measured experimentally with in vitro cascade impaction studies...
June 1, 2018: AAPS PharmSciTech
Carolin Korte, Julian Quodbach
3D printing evolved as a promising technique to improve individualization of drug therapy. In particular, when printing sustained release solid dosage forms, as for instance implants, inserts, and also tablets, estimation of the drug release profile in vivo is necessary. In most cases, corresponding analyses cannot be performed at hospital or community pharmacies. Therefore, the present study aimed to develop a sustained release drug delivery system produced via 3D printing, which allows dose adaption and estimation of drug release at the same time...
May 31, 2018: AAPS PharmSciTech
Daniel J Ellenberger, Dave A Miller, Robert O Williams
Due to the high number of poorly soluble drugs in the development pipeline, novel processes for delivery of these challenging molecules are increasingly in demand. One such emerging method is KinetiSol, which utilizes high shear to produce amorphous solid dispersions. The process has been shown to be amenable to difficult to process active pharmaceutical ingredients with high melting points, poor organic solubility, or sensitivity to heat degradation. Additionally, the process enables classes of polymers not conventionally processable due to their high molecular weight and/or poor organic solubility...
May 30, 2018: AAPS PharmSciTech
Chaojie Sun, Yun Gui, Rongfeng Hu, Jiayi Chen, Bin Wang, Yuxing Guo, Wenjie Lu, Xiangjiang Nie, Qiang Shen, Song Gao, Wenyou Fang
The study was performed aiming to enhance the solubility and oral bioavailability of poorly water-soluble drug osthole by formulating solid self-microemulsifying drug delivery system (S-SMEDDS) via spherical crystallization technique. Firstly, the liquid self-microemulsifying drug delivery system (L-SMEDDS) of osthole was formulated with castor oil, Cremophor RH40, and 1,2-propylene glycol after screening various lipids and emulsifiers. The type and amount of polymeric materials, good solvents, bridging agents, and poor solvents in S-SMEDDS formulations were further determined by single-factor study...
May 29, 2018: AAPS PharmSciTech
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