2,603 results match your criteria AAPS PharmSciTech[Journal]


New Approach for the Application of USP Apparatus 3 in Dissolution Tests: Case Studies of Three Antihypertensive Immediate-Release Tablets.

AAPS PharmSciTech 2018 Jun 22. Epub 2018 Jun 22.

Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Campus Reitor João David Ferreira Lima, Trindade, Florianópolis, Santa Catarina, 88040-970, Brazil.

The USP Apparatus 3 is a compendial dissolution Apparatus that has been mainly used to assess the performance of modified-release drug products. However, this Apparatus can be applied to dissolution testing of immediate-release tablets as well, with several advantages such as lower consumption of dissolution media, reduced setup time in quality control routine, and minimized hydrodynamic issues. In this work, three immediate-release (IR) tablets containing antihypertensive drugs of different Biopharmaceutic Classification System (BCS) classes were evaluated in order to assess the possible interchangeability between the official dissolution method using typical USP Apparatus 1 or 2 and the proposed methods using USP Apparatus 3. Read More

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The Effect of Inkjet Printing over Polymeric Films as Potential Buccal Biologics Delivery Systems.

AAPS PharmSciTech 2018 Jun 22. Epub 2018 Jun 22.

Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santos Dumont 964, 4to piso, Oficina # 09, Independencia, 8380494, Santiago, Chile.

The buccal mucosa appears as a promissory route for biologic drug administration, and pharmaceutical films are flexible dosage forms that can be used in the buccal mucosa as drug delivery systems for either a local or systemic effect. Recently, thin films have been used as printing substrates to manufacture these dosage forms by inkjet printing. As such, it is necessary to investigate the effects of printing biologics on films as substrates in terms of their physical and mucoadhesive properties. Read More

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Paul B. Myrdal, Ph.D. (June 25, 1967-May 19, 2018).

AAPS PharmSciTech 2018 Jun 21. Epub 2018 Jun 21.

Johnson & Johnson, Molecular Pharmaceutics and Drug Delivery, Austin, Texas, USA.

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Novel Extended-Release Multiple-Unit System of Imidafenacin Prepared by Fluid-Bed Coating Technique.

AAPS PharmSciTech 2018 Jun 21. Epub 2018 Jun 21.

College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul, 156-756, South Korea.

The objective of this study was to formulate once-a-day extended-release (ER) pellet system of imidafenacin (IDN), a recently approved urinary antispasmodic agent with twice-a-day dosing regimen. The sugar sphere pellets were firstly layered with IDN and hypromellose and then coated with Eudragit RS (copolymers of acrylic and methacrylic acid esters), employed as a release modifier, using a fluid-bed coater. Solid-state characterizations using solid-state X-ray diffraction and differential scanning calorimeter indicated that the antispasmodic agent was homogeneously layered onto the pellets in an amorphous state. Read More

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Effect of Complexes and Microemulsions on the Permeability of Drugs: Determination Using a New Biomimetic Artificial Membrane.

AAPS PharmSciTech 2018 Jun 19. Epub 2018 Jun 19.

Unidad de Investigación y Desarrollo en Ciencia y Tecnología Farmacéutica (UNITEFA-CONICET), Departamento de Farmacia, Facultad de Ciencias Químicas-Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina.

The aim of this work was to predict the permeability of two model drugs, sulfamerazine (SMR) and indomethacin (INM), and to determine the effect on their apparent permeabilities by complexation with cyclodextrins and/or meglumine or incorporation in microemulsions. Permeation experiments were performed using two-chamber diffusion cells with a new composition of bio-mimetic membrane composed of 80% of Lipoid® S100 and 20% of cholesterol in n-octanol 10% w/w solution, at 37 ± 0.5°C and 14,000 rpm. Read More

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Influence of Polymers on the Physical and Chemical Stability of Spray-dried Amorphous Solid Dispersion: Dipyridamole Degradation Induced by Enteric Polymers.

AAPS PharmSciTech 2018 Jun 18. Epub 2018 Jun 18.

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.

Amorphous solid dispersions (ASDs) are inherently unstable because of high internal energy. Evaluating physical and chemical stability during the process and storage is essential. Numerous researches have demonstrated how polymers influence the drug precipitation and physical stability of ASDs, while the influence of polymers on the chemical stability of ASDs is often overlooked. Read More

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Getting the Jump on the Development of Bullfrog Oil Microemulsions: a Nanocarrier for Amphotericin B Intended for Antifungal Treatment.

AAPS PharmSciTech 2018 Jun 18. Epub 2018 Jun 18.

Graduate Program in Pharmaceutical Sciences, Dispersed Systems Laboratory (LaSid), Federal University of Rio Grande do Norte (UFRN), Rua General Gustavo Cordeiro de Faria, S/N, Natal, RN, 59012-570, Brazil.

Amphotericin B (AmB), a potent antifungal drug, presents physicochemical characteristics that impair the development of suitable dosage forms. In order to overcome the AmB insolubility, several lipid carriers such as microemulsions have been developed. In this context, the bullfrog oil stands out as an eligible oily phase component, since its cholesterol composition may favor the AmB incorporation. Read More

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Co-Processed Excipients for Dispersible Tablets-Part 1: Manufacturability.

AAPS PharmSciTech 2018 Jun 18. Epub 2018 Jun 18.

GlaxoSmithKline, R&D, Park Road, Ware, Herts, SG12 0DP, UK.

Co-processed excipients may enhance functionality and reduce drawbacks of traditional excipients for the manufacture of tablets on a commercial scale. The following study aimed to characterise a range of co-processed excipients that may prove suitable for dispersible tablet formulations prepared by direct compression. Co-processed excipients were lubricated and compressed into 10. Read More

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June 2018
1 Read

Imidazole-Bearing Polymeric Micelles for Enhanced Cellular Uptake, Rapid Endosomal Escape, and On-demand Cargo Release.

AAPS PharmSciTech 2018 Jun 18. Epub 2018 Jun 18.

School of Pharmaceutical Science and Technology, Tianjin Key Laboratory for Modern Drug Delivery and High Efficiency, and Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin University, 92 Weijin Road, Nankai District, Tianjin, 300072, China.

The complex design of multifunctional nanomedicine is beneficial to overcome the multiple biological barriers of drug delivery, but it also presents additional hurdles to clinical translation (e.g., scaling-up and quality control). Read More

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Flutamide-Loaded Zein Nanocapsule Hydrogel, a Promising Dermal Delivery System for Pilosebaceous Unit Disorders.

AAPS PharmSciTech 2018 Jun 7. Epub 2018 Jun 7.

Industrial Pharmacy Department, Faculty of Pharmacy, Alexandria University, 1 Midan Alkhartoom square, Alazarita, Alexandria, Egypt.

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. Read More

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June 2018
2 Reads

A Modified In Situ Method to Determine Release from a Complex Drug Carrier in Particle-Rich Suspensions.

AAPS PharmSciTech 2018 Jun 6. Epub 2018 Jun 6.

Department of Pharmacy, Uppsala Biomedical Center, Uppsala University, BMC, P.O. Box 580, SE-751 23, Uppsala, Sweden.

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. Read More

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June 2018
3 Reads

Physiologically Based Absorption Modeling of Salts of Weak Bases Based on Data in Hypochlorhydric and Achlorhydric Biorelevant Media.

AAPS PharmSciTech 2018 Jun 5. Epub 2018 Jun 5.

Department of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, 15784, Zografou, Greece.

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. Read More

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June 2018
1 Read

Spray-Dried Proliposome Microparticles for High-Performance Aerosol Delivery Using a Monodose Powder Inhaler.

AAPS PharmSciTech 2018 Jun 5. Epub 2018 Jun 5.

Research Planning and Development, Office of Vice President for Research and Graduate Studies, Qatar University, P.O. Box 2713, Doha, Qatar.

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. Read More

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June 2018
2 Reads

Industrial Development of a 3D-Printed Nutraceutical Delivery Platform in the Form of a Multicompartment HPC Capsule.

AAPS PharmSciTech 2018 Jun 5. Epub 2018 Jun 5.

Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "Maria Edvige Sangalli", Università degli Studi di Milano, via G. Colombo 71, 20133, Milan, Italy.

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. Read More

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June 2018
4 Reads

Effects of Dendrimer-Like Biopolymers on Physical Stability of Amorphous Solid Dispersions and Drug Permeability Across Caco-2 Cell Monolayers.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907-2091, USA.

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. Read More

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June 2018
2 Reads

Unstructured Formulation Data Analysis for the Optimization of Lipid Nanoparticle Drug Delivery Vehicles.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548, Coimbra, Portugal.

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. Read More

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June 2018
2 Reads

Investigating the Physicochemical Stability of Highly Purified Darunavir Ethanolate Extracted from PREZISTA® Tablets.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

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. Read More

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June 2018
2 Reads

Is Vitamin D Transdermal Formulation Feasible? An Ex Vivo Skin Retention and Permeation.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Pharmacy, University of São Paulo (USP), Sao Paulo, Brazil.

Vitamin D 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 D. Read More

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June 2018
1 Read

Generation of a Weakly Acidic Amorphous Solid Dispersion of the Weak Base Ritonavir with Equivalent In Vitro and In Vivo Performance to Norvir Tablet.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

College of Pharmacy, The University of Texas at Austin, 1 University Station, Campus Mail Code A1902, Austin, Texas, 78712, USA.

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. Read More

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June 2018
4 Reads

Isolation, Formulation, and Efficacy Enhancement of Morin Emulsified Carriers Against Lung Toxicity in Rats.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Biochemistry Department, Faculty of Pharmacy, October 6 University, Giza, Egypt.

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 HgCl-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. Read More

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June 2018
4 Reads

Co-delivery of Metformin and Paclitaxel Via Folate-Modified pH-Sensitive Micelles for Enhanced Anti-tumor Efficacy.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan Province, China.

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). Read More

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June 2018
2 Reads

Characterization of Lipid-Based Lyotropic Liquid Crystal and Effects of Guest Molecules on Its Microstructure: a Systematic Review.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, Anhui Province, China.

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 (Q), or hexagonal (H) 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. Read More

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June 2018
3 Reads

Preparation and Optimization of Fast-Disintegrating Tablet Containing Naratriptan Hydrochloride Using D-Optimal Mixture Design.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Pharmaceutics, Faculty of Pharmacy, Helwan University, Cairo, Egypt.

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 (X), hydrolyzed gelatin (X), glycine (X), and mannitol (X) of total solid material (TSM) w/w. The effect of the relative proportion of each component was determined on friability (Y), hardness (Y), and in vitro disintegration time (Y), which was then applied for formulation optimization. Read More

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June 2018
2 Reads

Transient Temperature Monitoring of Pharmaceutical Tablets During Compaction Using Infrared Thermography.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Mechanical and Aerospace Engineering, Rutgers University, 98 Brett Rd., Piscataway, New Jersey, 08854, USA.

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. Read More

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June 2018
2 Reads

Investigation of Cyclodextrin-Based Nanosponges for Solubility and Bioavailability Enhancement of Rilpivirine.

AAPS PharmSciTech 2018 Jun 4. Epub 2018 Jun 4.

Department of Chemistry, University of Torino, Torino, Italy.

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%). Read More

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June 2018
3 Reads

Effects of Formulation Variables on Lung Dosimetry of Albuterol Sulfate Suspension and Beclomethasone Dipropionate Solution Metered Dose Inhalers.

AAPS PharmSciTech 2018 Jun 1. Epub 2018 Jun 1.

Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD, USA.

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. These commercial MDIs, utilized as model systems, provided mid-points for a design of experiments (DoE) plan to manufacture multiple suspension and solution MDI formulations. Read More

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June 2018
2 Reads

3D-Printed Network Structures as Controlled-Release Drug Delivery Systems: Dose Adjustment, API Release Analysis and Prediction.

AAPS PharmSciTech 2018 May 31. Epub 2018 May 31.

Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University, Universitätsstr. 1, 40225, Düsseldorf, Germany.

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. Read More

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May 2018
4 Reads

Expanding the Application and Formulation Space of Amorphous Solid Dispersions with KinetiSol®: a Review.

AAPS PharmSciTech 2018 May 30. Epub 2018 May 30.

College of Pharmacy, The University of Texas at Austin, 1 University Station, Campus Mail Code A1902, Austin, Texas, 78712, USA.

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. Read More

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May 2018
4 Reads

Preparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Key Laboratory of Xin'an Medicine, Ministry of Education, Anhui Province, Key Laboratory of R&D of Chinese Medicine, Anhui University of Traditional Chinese Medicine, Hefei, 230038, Anhui, People's Republic of China.

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. Read More

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May 2018
5 Reads

Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, End of 90th st, Cairo, Egypt.

Ondansetron hydrochloride (OND) is commonly used for management of postoperative and chemotherapeutic-induced nausea and vomiting. It suffers from low bioavailability (60%) and rapid elimination (t; 3-4 h). The current work aimed to develop OND-loaded bilosomes as a promising transdermal delivery system capable of surmount drug limitations. Read More

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May 2018
2 Reads

Application of Solvent Parameters for Predicting Organogel Formation.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

School of Pharmacy, Shenyang Pharmaceutical University, 85 Hongliu Road, Benxi, 117004, People's Republic of China.

Solvents, accounting the majority of the organogel system, have a tremendous impact on the characteristics of gels. To date, there is a large variety of organogel systems; relatively few have been investigated in the field of structure-solvent correlation. Here, a series of solvent parameters were applied to explore the role of solvent effect on network forming and gel property, intending to build the connection between the precise solvent parameter and gel property. Read More

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May 2018
3 Reads

Solving the Delivery Problems of Triclabendazole Using Cyclodextrins.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Instituto de Química de Rosario, Consejo Nacional de Investigaciones Científicas y Tecnológicas, Suipacha 531, 2000, Rosario, Argentina.

Triclabendazole is the first-line drug of choice to treat and control fasciolasis, a neglected parasitic human disease. It is a class II/IV compound according to the Biopharmaceutics Classification System. Thus, the aim of this study was to improve aqueous solubility and dissolution rate of triclabendazole complexed with 2-hydroxylpropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) at 1:1 and 1:2 M ratio. Read More

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May 2018
2 Reads

Scale up of Semisolid Dosage Forms Manufacturing Based on Process Understanding: from Lab to Industrial Scale.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, 3584 CG, Utrecht, The Netherlands.

The scale up of production processes is a major challenge in pharmaceutical industry. Using a quality by design approach, upscaling can be based on the design space, which can be assessed on a small scale. In a previous study, the critical process parameters were identified by a definitive screening design on cetomacrogol ointment. Read More

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May 2018
2 Reads

A Novel Colon-Specific Osmotic Pump Capsule of Panax notoginseng Saponins (PNS): Formulation, Optimization, and In Vitro-In Vivo Evaluation.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Key Laboratory of Xin'an Medicine, Ministry of Education, Anhui Province, Key Laboratory of R&D of Chinese Medicine, Anhui University of Chinese Medicine, Hefei, 230038, Anhui, People's Republic of China.

In the current study, a novel colon-specific osmotic pump capsule of Panax notoginseng saponins was developed to achieve colon-specific release, a zero-order, thus to promote the efficacy of Panax notoginseng saponins. The capsule was assembled using a semi-permeable capsule shell with contents including Panax notoginseng saponins, sodium chloride (NaCl), and Ludipress. The semipermeable membrane was made of cellulose acetate (CA), along with polyethylene glycol (PEG) 6000 for flexibility and strength, and Eudragit® S100 for colon-specific targeting. Read More

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May 2018
2 Reads

Influence of Postprandial Intragastric Pressures on Drug Release from Gastroretentive Dosage Forms.

AAPS PharmSciTech 2018 May 29. Epub 2018 May 29.

Department of Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport, Institute of Pharmacy, University of Greifswald, Felix-Hausdorff-Straße 3, 17487, Greifswald, Germany.

Despite extensive research in the field of gastroretentive dosage forms, this "holy grail" of oral drug delivery yet remained an unmet goal. Especially under fasting conditions, the reproducible retention of dosage forms in the stomach seems to be an impossible task. This is why such systems are often advised to be taken together with food. Read More

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May 2018
2 Reads

Development of a Topical 48-H Release Formulation as an Anti-scarring Treatment for Deep Partial-Thickness Burns.

AAPS PharmSciTech 2018 May 11. Epub 2018 May 11.

Dental and Craniofacial Trauma Research and Tissue Regeneration, US Army Institute of Surgical Research, 3650 Chambers Pass, JBSA Fort Sam, Houston, Texas, 78234-7767, USA.

The purpose of this study was to develop pirfenidone (PF) ointment formulations for a dose finding study in the prophylactic treatment of deep partial-thickness burns in a mouse model. A preformulation study was performed to evaluate the solubility of PF in buffers and different solvents and its stability. Three different formulations containing 1, 3. Read More

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Improving the Stability and the Pharmaceutical Properties of Norfloxacin Form C Through Binary Complexes with β-Cyclodextrin.

AAPS PharmSciTech 2018 May 10. Epub 2018 May 10.

Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina.

Norfloxacin, an antibiotic that exists in different solid forms, has very unfavorable properties in terms of solubility and stability. Binary complexes of norfloxacin, in the solid form C, and β-cyclodextrin were procured by the kneading method and physical mixture. Their effect on the solubility, the dissolution rate, and the chemical and physical stability of norfloxacin was evaluated. Read More

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May 2018
3 Reads

Correction to: First Development, Optimization, and Stability Control of a Pediatric Oral Atenolol Formulation.

AAPS PharmSciTech 2018 Apr 16. Epub 2018 Apr 16.

Área Análisis de Medicamentos, Departamento Química Orgánica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000, Rosario, Argentina.

In the INTRODUCTION section, Atenolol is defined in parenthesis as (ATN, Fig. 1.) The correct definition is (ATN). Read More

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Characterization and In Vitro Permeation Study of Cubic Liquid Crystal Containing Sinomenine Hydrochloride.

AAPS PharmSciTech 2018 May 8. Epub 2018 May 8.

School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, Jiangsu Province, China.

This study developed a new transdermal delivery system for the improved delivery of sinomenine hydrochloride (SH). The delivery system utilized the advantages of lyotropic liquid crystals (LLC) creating an adaptable system that offers a variety of options for the field of transdermal delivery. The formulation was prepared, characterized, and evaluated for its skin penetration in vitro. Read More

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Spray-Freeze Drying: a Suitable Method for Aerosol Delivery of Antibodies in the Presence of Trehalose and Cyclodextrins.

AAPS PharmSciTech 2018 May 8. Epub 2018 May 8.

Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

We aimed to prepare spray-freeze-dried powder of IgG considering physicochemical stability and aerodynamic aspects. Spray-freeze drying (SFD) exposes proteins to various stresses which should be compensated by suitable stabilizers. The competence of cyclodextrins (CDs), namely beta-cyclodextrin (βCD) and hydroxypropyl βCD (HPβCD), at very low concentrations, was investigated in the presence of separate mannitol- and trehalose-based formulations. Read More

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Editorial for Theme Issue: Applications of KinetiSol Dispersing for Advanced Amorphous Solid Dispersions.

Authors:
Dave A Miller

AAPS PharmSciTech 2018 May 8. Epub 2018 May 8.

DisperSol Technologies, Georgetown, Texas, USA.

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Zein as a Pharmaceutical Excipient in Oral Solid Dosage Forms: State of the Art and Future Perspectives.

AAPS PharmSciTech 2018 May 7. Epub 2018 May 7.

School of Pharmacy, University of Camerino, 62032, Camerino, MC, Italy.

Zein is the main storage protein of corn and it has several industrial applications. Mainly in the last 10-15 years, zein has emerged as a potential pharmaceutical excipient with unique features. Zein is a natural, biocompatible and biodegradable material produced from renewable sources. Read More

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Transfer Behavior of the Weakly Acidic BCS Class II Drug Valsartan from the Stomach to the Small Intestine During Fasted and Fed States.

AAPS PharmSciTech 2018 May 7. Epub 2018 May 7.

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, P.O. Box 130, Amman, 11733, Jordan.

The objective of this study was to investigate the transfer behavior of the weakly acidic BCS class II drug valsartan from the stomach to the small intestine during fasted and fed states. An in vitro transfer model previously introduced by Kostewicz et al. (J Pharm Pharmacol 56(1):43-51, 2004) based on a syringe pump and a USP paddle apparatus was used to determine the concentration profiles of valsartan in the small intestine. Read More

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May 2018
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Investigation of Carrageenan Aerogel Microparticles as a Potential Drug Carrier.

AAPS PharmSciTech 2018 May 7. Epub 2018 May 7.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.

Carrageenan is an anionic polysaccharide offering many advantages to be used in drug delivery applications. These include availability, thermo-stability, low toxicity, and encapsulating properties. Combination of these properties with aerogel properties like large surface area and porosity make them an ideal candidate for drug adsorption and delivery applications. Read More

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May 2018
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Formulation, Characterization, and Optimization of Captopril Fast-Dissolving Oral Films.

AAPS PharmSciTech 2018 May 4. Epub 2018 May 4.

Department of Biomedical Engineering, Faculty of Chemical Engineering, Tarbiat Modares University, P.O. Box 14115-114, Tehran, Iran.

This work aimed to using optimization study to formulate a patient-friendly captopril fast-dissolving oral film with satisfactory disintegration time. Films were made with pullulan and hydroxypropyl methyl cellulose (HPMC) by using the solvent-casting method. Cellulose nanofiber (CNF) was used as a compatibilizer and glycerine was used as a plasticizer. Read More

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May 2018
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Dapsone-Loaded Invasomes as a Potential Treatment of Acne: Preparation, Characterization, and In Vivo Skin Deposition Assay.

AAPS PharmSciTech 2018 May 3. Epub 2018 May 3.

Department of Industrial Pharmacy and Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Dapsone (DPS) is a unique sulfone with antibiotic and anti-inflammatory activity. Owing to its dual action, DPS has a great potential to treat acne. Topical DPS application is expected to be effective in treatment of mild to moderate acne conditions. Read More

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Therapeutic Effect of a Novel Nano-Drug Delivery System on Membranous Glomerulonephritis Rat Model Induced by Cationic Bovine Serum.

AAPS PharmSciTech 2018 May 3. Epub 2018 May 3.

Department of Pharmaceutics, School of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.

In order to explore a novel high efficacy drug delivery system for membranous glomerulonephritis (MGN), a complex chronic inflammation, methylprednisolone bovine serum albumin nanoparticles (ME BSA NPs) were designed. The nanoparticles were prepared by desolvation-chemical crosslinking method and its physicochemical characterizations were conducted. The experimental MGN rat models induced by cationic bovine serum albumin were established by a modified Border's method and applied in the pharmacodynamics study of ME BSA NPs. Read More

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Optimization of a Coupling Process for Insulin Degludec According to a Quality by Design (QbD) Paradigm.

AAPS PharmSciTech 2018 May 3. Epub 2018 May 3.

Pharmaceutical Informatics Institute, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

This case study described a successful application of the quality by design (QbD) principles to a coupling process development of insulin degludec. Failure mode effects analysis (FMEA) risk analysis was first used to recognize critical process parameters (CPPs). Five CPPs, including coupling temperature (Temp), pH of desB30 solution (pH), reaction time (Time), desB30 concentration (Conc), and molar equivalent of ester per mole of desB30 insulin (MolE), were then investigated using a fractional factorial design. Read More

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May 2018
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Ceramide-Fabricated Co-Loaded Liposomes for the Synergistic Treatment of Hepatocellular Carcinoma.

AAPS PharmSciTech 2018 Apr 30. Epub 2018 Apr 30.

School of Pharmaceutical Sciences, Key Laboratory of Chemical Biology (Ministry of Education), Shandong University, 44 Wen Hua Xi Road, Ji'nan, 250012, Shandong Province, People's Republic of China.

Combination therapy is one of the important methods to improve therapeutic effect on the treatment of hepatocellular carcinoma (HCC). Sorafenib (SF) is a canonical US Food and Drug Administration-approved multikinase molecule inhibitor against HCC. However, therapeutic benefit with Sorafenib alone was usually unsatisfactory. Read More

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April 2018
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Dry Gel Containing Optimized Felodipine-Loaded Transferosomes: a Promising Transdermal Delivery System to Enhance Drug Bioavailability.

AAPS PharmSciTech 2018 Apr 30. Epub 2018 Apr 30.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El- Eini St., Cairo, Egypt.

Felodipine has a very low bioavailability due to first-pass metabolism. The aim of this study was to enhance its bioavailability by transdermal application. Felodipine-loaded transferosomes were prepared by thin-film hydration using different formulation variables. Read More

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April 2018
2 Reads