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AAPS PharmSciTech

Rina Suzuki, Yutaka Inoue, Sontaya Limmatvapirat, Isamu Murata, Ikuo Kanamoto
The aim of this study was to prepare inclusion complexes of hinokitiol (HT)/α-cyclodextrin (α-CD) and HT/β-cyclodextrin (β-CD) by cogrinding and to evaluate the differences in their formation. The physical properties of the preparation were evaluated by Job's plot, phase solubility studies, differential scanning calorimetry, powder X-ray diffraction, solid fluorescence spectra, and infrared absorption spectra. Intermolecular interaction in the solid state was confirmed to be in the ratios HT/α-CD = 1/2 and HT/β-CD = 1/1...
March 15, 2017: AAPS PharmSciTech
Minh Nguyet Pham, Toi Van Vo, Van-Thanh Tran, Phuong Ha-Lien Tran, Thao Truong-Dinh Tran
Microemulsion has the potentials to enhance dissolution as well as facilitate absorption and permeation of poorly water-soluble drugs through biological membranes. However, its application to govern a controlled release buccal delivery for local treatment has not been discovered. The aim of this study is to develop microemulsion-based mucoadhesive wafers for buccal delivery based on an incorporation of the microemulsion with mucoadhesive agents and mannitol. Ratio of oil to surfactant to water in the microemulsion significantly impacted quality of the wafers...
March 15, 2017: AAPS PharmSciTech
Avadhesh Singh Kushwaha, P Sharma, H N Shivakumar, C Rappleye, A Zukiwski, S Proniuk, S Narasimha Murthy
AR-12 is a novel small molecule with broad spectrum antifungal activity. Recently, AR-12 was found to be highly active against Trichophyton rubrum, one of the predominantly responsible organisms that cause onychomycosis. The primary objective of this project was to investigate the ability of AR-12 to penetrate into and across the human nail plate followed by improving its trans-ungual permeation using different penetration enhancers. TranScreen-N™, a high throughput screening method was utilized to explore the potential nail penetration enhancers to facilitate the drug delivery through the nail...
March 13, 2017: AAPS PharmSciTech
Lorina Bisharat, Diego R Perinelli, Alberto Berardi, Giulia Bonacucina, Serena Logrippo, Feras W Darwish Elhajji, Marco Cespi, Giovanni F Palmieri
The immersion cell is an in vitro performance test of drug release from semisolids. Several studies made use of immersion cells to investigate drug release from thermosensitive Poloxamer-based gels; however, specifications on the parameter setting are not yet available. Therefore, the aim of this study was to evaluate the influence of testing parameters on tramadol (a model drug) release, release rate, and dissolution efficiency (DE) from Poloxamer gels, using immersion cells. The thermosensitive gelling formulation showed batch-to-batch uniformity of gelling behavior, drug content, and drug release...
March 13, 2017: AAPS PharmSciTech
Katherina Fernández, Marlene Roeckel, Edgardo Canales, Javiera Dumont
Proanthocyanidins (PAs) have several bioactivities, but they are unstable in the digestive tract and possess low bioavailability. Nanoencapsulation stabilizes these compounds for oral administration. The intestinal absorption of grape seed and skin extracts, and the poly-lactic acid (PLA) nanoparticles loaded with such extracts was modeled, taking into consideration physicochemical process parameters, evaluating the PAs concentration profile in the human small intestine. Density (ρ), solubility, viscosity (μ), diffusion coefficient (D), and the global mass transfer coefficient (K) for both substrates were estimated, simulating their passing from the intestine into the blood at 37°C...
March 10, 2017: AAPS PharmSciTech
Kai Chen, Yanyan Wang, Xiumei Gai, Haiying Wang, Yuenan Li, Haoyang Wen, Weisan Pan, Xinggang Yang
The objective of this study was to design a time-controlled pulsatile release (TCPR) system containing propranolol (PNH) as an active pharmaceutical ingredient. Here, the developed dosage forms were coated with hydroxypropyl-methylcellulose (HPMC) and other excipients as barrier layer using dry-coated technology. The influence of HPMC, microcrystalline cellulose (MCC), and lactose in the outer coating and the coating weight on drug release were investigated. Then, a three-factor, five-level central composite design (CCD) and response surface method were used to optimize the formula of the coating...
March 9, 2017: AAPS PharmSciTech
Ebru Altuntaş, Gülgün Yener
The purpose of the present work was to develop a mucoadhesive thermoreversible nasal gel with a tailored gelling temperature to provide the prolonged contact between mometasone furoate and the nasal mucosa and in order to prevent drainage of the formulation. For this purpose, in situ gel containing a thermogelling polymer poloxamer 407 (Pluronic® F-127) and a mucoadhesive polymer Carbopol® 974P NF was prepared. In this content, formulations were designed to have gelation temperature below 34°C to obtain gelation at intranasal cavity...
March 9, 2017: AAPS PharmSciTech
Khalil Sakeer, Pompilia Ispas-Szabo, Mircea Alexandru Mateescu
A new class of starch derivatives carrying cationic and anionic functional groups was developed aiming to provide an alternative for the formulation of highly soluble drugs. The new ampholytic starch derivatives were synthesized in two steps; first the CarboxyMethyl (CM) groups were grafted on starch chains followed by introduction of AminoEthyl (AE) groups. The final product, CarboxyMethyl-AminoEthyl-Starch (CM-AE-St), could be obtained in different degrees of substitution by varying the number of CM and AE groups...
March 7, 2017: AAPS PharmSciTech
Abeer Khattab, Nashwah Zaki
The purpose of our investigation was to develop and optimize the drug entrapment efficiency and bioadhesion properties of mucoadhesive chitosan microspheres containing ranitidine HCl prepared by an ionotropic gelation method as a gastroretentive delivery system; thus, we improved their protective and therapeutic gastric effects in an ulcer model. A 3 × 2(2) full factorial design was adopted to study the effect of three different factors, i.e., the type of polymer at three levels (chitosan, chitosan/hydroxypropylmethylcellulose, and chitosan/methylcellulose), the type of solvent at two levels (acetic acid and lactic acid), and the type of chitosan at two levels (low molecular weight (LMW) and high molecular weight (HMW))...
March 7, 2017: AAPS PharmSciTech
Yan Liang Fan, Han Wei Hou, Hui Min Tay, Wei Mei Guo, Per-Olof Berggren, Say Chye Joachim Loo
Rapamycin is commonly used in chemotherapy and posttransplantation rejection suppression, where sustained release is preferred. Conventionally, rapamycin has to be administered in excess due to its poor solubility, and this often leads to cytotoxicity and undesirable side effects. In addition, rapamycin has been shown to be hydrolytically unstable, losing its bioactivity within a few hours. The use of drug delivery systems is hypothesized to preserve the bioactivity of rapamycin, while providing controlled release of this otherwise potent drug...
March 1, 2017: AAPS PharmSciTech
E Sayed, R Haj-Ahmad, K Ruparelia, M S Arshad, M-W Chang, Z Ahmad
Innovative methods and materials have been developed to overcome limitations associated with current drug delivery systems. Significant developments have led to the use of a variety of materials (as excipients) such as inorganic and metallic structures, marking a transition from conventional polymers. Inorganic materials, especially those possessing significant porosity, are emerging as good candidates for the delivery of a range of drugs (antibiotics, anticancer and anti-inflammatories), providing several advantages in formulation and engineering (encapsulation of drug in amorphous form, controlled delivery and improved targeting)...
February 28, 2017: AAPS PharmSciTech
Nilesh Desai, Ravindra Purohit
Clopidogrel bisulfate (CBS) is antiplatelet drug and it is becoming a drug of choice in the treatment and management of prevention of heart attacks and strokes. CBS is stable and soluble in acidic pH; therefore, retention in stomach for prolonged period appears to be beneficial for controlling the bioavailability. The gastroretentive osmotic system (GROS) facilitates prolonged retention of drug in stomach and provides zero-order drug release. A complex formulation like GROS poses many challenges, and QbD tools can help in designing robust formulation which takes all aspects of product and process development in order to deliver a robust product...
February 28, 2017: AAPS PharmSciTech
Nicole S Mendonsa, Priyanka Thipsay, Dong Wuk Kim, Scott T Martin, Michael A Repka
As the buccal route of administration has the ability to avoid the GI tract and first-pass effect by directing the absorption toward the cheek area, the bioavailability of BCS class III drugs can be increased through this route. Only a handful of studies have been conducted using oleic acid as a permeation enhancer in any transbuccal drug delivery system. Therefore, the objectives of this novel study were to develop a buccal tablet using two concentrations of oleic acid for a model BCS class III drug via hot-melt extrusion technology and to investigate the effects of oleic acid on the physicochemical properties of the tablet...
February 28, 2017: AAPS PharmSciTech
Menglu Xu, Yulin Chen, Parikshit Banerjee, Li Zong, Lei Jiang
Specific and effective delivery of DNA vaccines into dendritic cells (DCs) to express antigens is a precondition for induction of immune responses. Construction of a new DNA vaccine delivery system with the ability of programmed gene transfection may achieve this objective. In this study, we successfully integrated dendritic lipopeptide, charge-reversible polymer, and APC-targeted material into DNA vaccine delivery system through layer-by-layer (LBL) assembly. By the means of adjusting the weight ratios and concentration ratios of components, stable complexes were formulated with a particle size of 256...
February 27, 2017: AAPS PharmSciTech
Tao Liu, Guili Yao, Xiaotian Liu, Haipeng Yin
The usage of downscaling technology for producing nanosuspensions/nanocrystals can be beneficial for formulation development, which has attracted increased attention recently. An ultra-small bead milling method (5 mg compound per batch, smallest scale to date) was tested to produce nanocrystals of four poorly soluble plant compounds, i.e., quercetin, rutin, resveratrol, and hesperidin. A particle size of ranged from 200 to 500 nm was obtained for nanosuspensions of four compounds and the stabilizer selection could be achieved within 2 h by using this ultra-small bead milling method...
February 27, 2017: AAPS PharmSciTech
Hannah D Stonewall, Haley M Kessinger, Abebe E Mengesha
The crystallization behavior and temperature-dependent phase transition of monoglycerides have been utilized to develop thermal-sensitive drug delivery systems. The presence of excess water has been reported to influence the phase transition. The present study investigates the effect of moisture on the thermal behavior of binary blends of monoglycerides. Various compositions (0-100 wt%) of glyceryl monooleate (GMO) and glyceryl monostearate (GMS) were prepared by fusion method, and exposed to varying relative humidity (RH) levels (0-100%)...
February 27, 2017: AAPS PharmSciTech
Shaimaa Elkadi, Samar Elsamaligy, Saleh Al-Suwayeh, Hanaa Mahmoud
The aim of this work was to develop self-nanoemulsifying liquisolid tablets (SNELT) to enhance the dissolution profile of poorly water-soluble simvastatin. SNELT present a unique technique of incorporating self-nanoemulsifying drug delivery systems (SNEDDS) into tablets. Optimized SNEDDS containing different oils, Cremophor(®) RH 40 (surfactant) and Transcutol(®) HP (co-surfactant), at different ratios, were used as liquid vehicles and loaded on carrier material, microcrystalline cellulose (MCC), and coating material, Cab-o-sil(®) H-5 (nanosize colloidal silicon dioxide) powders at different loading factors (L f ) and fixed excipient ratio (R = 20)...
February 24, 2017: AAPS PharmSciTech
Francisca Mano, Marta Martins, Isabel Sá-Nogueira, Susana Barreiros, João Paulo Borges, Rui L Reis, Ana Rita C Duarte, Alexandre Paiva
Fast-dissolving delivery systems (FDDS) have received increasing attention in the last years. Oral drug delivery is still the preferred route for the administration of pharmaceutical ingredients. Nevertheless, some patients, e.g. children or elderly people, have difficulties in swallowing solid tablets. In this work, gelatin membranes were produced by electrospinning, containing an encapsulated therapeutic deep-eutectic solvent (THEDES) composed by choline chloride/mandelic acid, in a 1:2 molar ratio. A gelatin solution (30% w/v) with 2% (v/v) of THEDES was used to produce electrospun fibers and the experimental parameters were optimized...
February 24, 2017: AAPS PharmSciTech
Namita Dalal, Ira S Buckner, Peter L D Wildfong
Cefuroxime axetil (CFA), an ester prodrug of cefuroxime exists as a pair of diastereoemers, namely isomer A and isomer B. To enable phase diagram construction, crystallization of the diastereomers of CFA from the commercially available amorphous drug substance was carried out. Isomer A was separated with a purity approaching 100% whereas the maximum purity of isomer B was 85% as confirmed by solution state proton NMR spectroscopy. The crystalline forms of isomer A and isomer B were confirmed as forms AI and BI, respectively, based on differential scanning calorimetry (DSC) analysis and powder X-ray diffraction...
February 22, 2017: AAPS PharmSciTech
Jin Wang, Ruimiao Chang, Yanan Zhao, Jiye Zhang, Ting Zhang, Qiang Fu, Chun Chang, Aiguo Zeng
Coamorphous systems using citric acid as a small molecular excipient were studied for improving physical stability and bioavailability of loratadine, a BCS class II drug with low water solubility and high permeability. Coamorphous loratadine-citric acid systems were prepared by solvent evaporation technique and characterized by differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy. Solid-state analysis proofed that coamorphous loratadine-citric acid system (1:1) was amorphous and homogeneous, had a higher T g over amorphous loratadine, and the intermolecular hydrogen bond interactions between loratadine and citric acid exist...
February 21, 2017: AAPS PharmSciTech
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