2,889 results match your criteria AAPS PharmSciTech[Journal]


Preformulation and Evaluation of Tofacitinib as a Therapeutic Treatment for Asthma.

AAPS PharmSciTech 2019 Apr 16;20(5):167. Epub 2019 Apr 16.

Department of Pharmaceutical Sciences, University of Arizona, Tucson, Arizona, USA.

Preformulation studies on tofacitinib citrate, a small molecule JAK3 specific inhibitor, have not been previously reported in literature. We therefore conducted several preformulation studies on tofacitinib citrate, and its free base, to better understand factors that affect its solubility, stability, and solid-state characteristics. Further, the results of the preformulation studies helped facilitate the development of a nebulized formulation of tofacitinib citrate for inhalational delivery to house dust mite allergen-challenged, BALB/c mice as a potential treatment for eosinophilic asthma. Read More

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http://link.springer.com/10.1208/s12249-019-1377-0
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http://dx.doi.org/10.1208/s12249-019-1377-0DOI Listing
April 2019
1 Read

Preparation, Characterization and Antioxidant Evaluation of Poorly Soluble Polyphenol-Loaded Nanoparticles for Cataract Treatment.

AAPS PharmSciTech 2019 Apr 15;20(5):163. Epub 2019 Apr 15.

School of Pharmacy and Health Professionals, Creighton University, Omaha, Nebraska, 68178, USA.

Cataract, one of the leading causes of blindness worldwide, is a condition in which complete or partial opacity develops in the lens of the eyes, thereby impairing vision. This study aimed to examine the potential therapeutic and protective effects of poorly soluble polyphenols like curcumin, resveratrol, and dibenzoylmethane, known to possess significant antioxidant activity. The polyphenols were loaded into novel lipid-cyclodextrin-based nanoparticles and characterized by particle size, polydispersity index, differential scanning calorimetry, thermogravimetric analysis, X-ray diffraction, scanning electron microscopy (SEM), entrapment efficiency, and release studies. Read More

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http://link.springer.com/10.1208/s12249-019-1379-y
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http://dx.doi.org/10.1208/s12249-019-1379-yDOI Listing
April 2019
1 Read

Poly (ɛ-Caprolactone) Nanoparticles with pH-Responsive Behavior Improved the In Vitro Antitumor Activity of Methotrexate.

AAPS PharmSciTech 2019 Apr 15;20(5):165. Epub 2019 Apr 15.

Department of Industrial Pharmacy, Universidade Federal de Santa Maria, Av. Roraima 1000, Santa Maria, RS, 97105-900, Brazil.

A promising approach to achieve a more efficient antitumor therapy is the conjugation of the active molecule to a nanostructured delivery system. Therefore, the main objective of this research was to prepare nanoparticles (NPs), with the polymer poly (ε-caprolactone) (PCL), as a carrier for the antitumor drug methotrexate (MTX). A pH-responsive behavior was obtained through conjugation of the amino acid-based amphiphile, 77KL, to the NP matrix. Read More

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http://dx.doi.org/10.1208/s12249-019-1372-5DOI Listing

Investigating the Effect of APAP Crystals on Tablet Behavior Manufactured by Direct Compression.

AAPS PharmSciTech 2019 Apr 16;20(5):168. Epub 2019 Apr 16.

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

In this work, the effect of API's (Active Pharmaceutical Ingredient) shape and size on tablet characteristics is investigated for high API dose formulation manufactured by direct compression. Three different classes of APAP (acetaminophen) are selected, and tablets are produced in both single and batch processes. After performing and comparing comprehensive series of standard characterization tests including hardness, dissolution, disintegration, and friability on the tablets, the test results show the relation between the quality of APAP tablets and the shape and size of the crystals. Read More

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http://dx.doi.org/10.1208/s12249-019-1369-0DOI Listing

In Vitro Drug Dissolution/Permeation Testing of Nanocarriers for Skin Application: a Comprehensive Review.

AAPS PharmSciTech 2019 Apr 15;20(5):164. Epub 2019 Apr 15.

Non-Destructive Biomedical and Pharmaceutical Research Centre, iPROMISE, Universiti Teknologi MARA Selangor, Puncak Alam Campus, 42300, Bandar Puncak Alam, Malaysia.

This review highlights in vitro drug dissolution/permeation methods available for topical and transdermal nanocarriers that have been designed to modulate the propensity of drug release, drug penetration into skin, and permeation into systemic circulation. Presently, a few of USFDA-approved in vitro dissolution/permeation methods are available for skin product testing with no specific application to nanocarriers. Researchers are largely utilizing the in-house dissolution/permeation testing methods of nanocarriers. Read More

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http://dx.doi.org/10.1208/s12249-019-1362-7DOI Listing

Development of MART for the Rapid Production of Nanostructured Lipid Carriers Loaded with All-Trans Retinoic Acid for Dermal Delivery.

AAPS PharmSciTech 2019 Apr 12;20(4):162. Epub 2019 Apr 12.

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.

All-trans retinoic acid (ATRA) has been regarded as a wonder drug for many dermatological complications; however, its application is limited due to the extreme irritation, and toxicity seen once it has sufficiently concentrated into the bloodstream from the skin. Thus, the present study was aimed to increase the entrapment of ATRA and minimize its transdermal permeation. ATRA incorporated within nanostructured lipid carriers (NLCs) were produced by a green and facile thin lipid-film based microwave-assisted rapid technique (MART). Read More

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http://dx.doi.org/10.1208/s12249-019-1307-1DOI Listing
April 2019
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Lesson Learnt from Recall of Valsartan and Other Angiotensin II Receptor Blocker Drugs Containing NDMA and NDEA Impurities.

AAPS PharmSciTech 2019 Apr 15;20(5):166. Epub 2019 Apr 15.

Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Building, Suite 159, College Station, Texas, 77843-1114, USA.

The presence of N-nitrosodimethylamine (NDMA) and N-nitrosodiethylamine (NDEA) impurities in angiotensin II receptor blocker (ARB) drugs containing tetrazole ring has triggered worldwide product recalls. The purpose of this article is to identify the potential gap area in current pharmaceutical industry practice that might have led to the NMDA and NDEA impurities escaping the drug manufacturer's and FDA's attention. The impact of process change was not adequately assessed by the manufacturer of contaminated APIs (active pharmaceutical ingredients), and potential for generation of mutagenic or other toxic impurities was not considered. Read More

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http://dx.doi.org/10.1208/s12249-019-1376-1DOI Listing

Lecithin Microemulsion Lipogels Versus Conventional Gels for Skin Targeting of Terconazole: In Vitro, Ex Vivo, and In Vivo Investigation.

AAPS PharmSciTech 2019 Apr 10;20(4):161. Epub 2019 Apr 10.

Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, 1-Azarita Square, Alexandria, Egypt.

Topical treatment of fungal infections has several superiorities over oral treatment. However, the greatest challenge for dermal delivery is the stratum corneum which is considered an effective barrier for penetration of most antifungal drugs into deeper skin layers. Terconazole (Tr), which is the first marketed triazole antifungal, was reported to be one of the most active azoles against vaginal candidiasis. Read More

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http://dx.doi.org/10.1208/s12249-019-1374-3DOI Listing
April 2019
1 Read

Evaluation of Hydrogenated Soybean Phosphatidylcholine Matrices Prepared by Hot Melt Extrusion for Oral Controlled Delivery of Water-Soluble Drugs.

AAPS PharmSciTech 2019 Apr 9;20(4):159. Epub 2019 Apr 9.

College of Pharmacy, Freie Universität Berlin, Berlin, Germany.

The aims of this study were to prepare hydrogenated soybean phosphatidylcholine (HSPC) matrices by hot melt extrusion and to evaluate resulting matrix potential to extend drug release in regard to drug loading and solubility for oral drug delivery of water-soluble drugs. The liquid crystalline nature of HSPC powder allowed its extrusion at 120°C, which was below its capillary melting point. Model drugs with a wide range of water solubilities (8, 20 and 240 mg/mL) and melting temperatures (160-270°C) were used. Read More

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http://dx.doi.org/10.1208/s12249-019-1366-3DOI Listing

Translational Multi-Disciplinary Approach for the Drug and Gene Delivery Systems for Cancer Treatment.

AAPS PharmSciTech 2019 Apr 9;20(4):160. Epub 2019 Apr 9.

Department of Pharmacy Sciences, School of Pharmacy and Health Professions, Creighton University, 2500 California Plaza, Omaha, Nebraska, 68178, USA.

Over the last several decades, nanoparticulate delivery systems have emerged as advanced drug and gene delivery tools for cancer therapy. However, their translation into clinical use still poses major challenges. Even though many innovative nanoparticulate approaches have shown very positive results both in vitro and in vivo, few of them have found a place in clinical practice. Read More

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http://link.springer.com/10.1208/s12249-019-1367-2
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http://dx.doi.org/10.1208/s12249-019-1367-2DOI Listing
April 2019
2 Reads

Insulin Mucoadhesive Liposomal Gel for Wound Healing: a Formulation with Sustained Release and Extended Stability Using Quality by Design Approach.

AAPS PharmSciTech 2019 Apr 8;20(4):158. Epub 2019 Apr 8.

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

The present study deals with the formulation of topical insulin for wound healing with extended stability and sustained release, by applying quality by design concepts. Insulin has been promoted as a promising therapeutic wound healing agent. Topical formulation of insulin faced major problems, as it cannot be delivered safely to the wound with a controlled rate. Read More

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http://dx.doi.org/10.1208/s12249-019-1363-6DOI Listing
April 2019
2 Reads
1.776 Impact Factor

Feedforward and Feedback Control of a Pharmaceutical Coating Process.

AAPS PharmSciTech 2019 Apr 1;20(4):157. Epub 2019 Apr 1.

Duquesne University Graduate School of Pharmaceutical Sciences, Pittsburgh, Pennsylvania, USA.

This work demonstrates the use of a combination of feedforward and feedback loops to control the controlled release coating of theophylline granules. Feedforward models are based on the size distribution of incoming granules and are used to set values for the airflow in the fluid bed processor and the target coat weight to be applied to the granules. The target coat weight of the granules is controlled by a feedback loop using NIR spectroscopy to monitor the progress of the process. Read More

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http://dx.doi.org/10.1208/s12249-019-1348-5DOI Listing
April 2019
1 Read

Systematically Optimized Imiquimod-Loaded Novel Hybrid Vesicles by Employing Design of Experiment (DoE) Approach with Improved Biocompatibility, Stability, and Dermatokinetic Profile.

AAPS PharmSciTech 2019 Mar 29;20(4):156. Epub 2019 Mar 29.

University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh, 160014, India.

The present research work explored the possibility of harnessing the benefits of vesicular carriers for overcoming imiquimod-associated complaints or side effects. Hybrid vesicles were prepared by the most common and easily scalable method, i.e. Read More

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http://dx.doi.org/10.1208/s12249-019-1331-1DOI Listing

Preparation and Evaluation of Mosapride Citrate Dual-Release Dry Suspension.

AAPS PharmSciTech 2019 Mar 28;20(4):155. Epub 2019 Mar 28.

College of Pharmacy, Nanjing Tech University, No. 30, Puzhu South Road, Nanjing, 211816, People's Republic of China.

In this paper, a novel formulation of dual-release dry suspension of mosapride citrate (DRDS-MC) was designed which can be quickly released in the stomach while having sustained-release effect. Co-grinding mixture of mosapride citrate (MC) together with L-HPC as hydrophilic excipient was prepared in order to improve the solubility of MC. The co-grinding mixture was characterized by solubility studies, DSC, X-RD, SEM, FTIR, and size distribution before the preparation of the DRDS-MC. Read More

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http://dx.doi.org/10.1208/s12249-019-1343-xDOI Listing
March 2019
1 Read

Optimization of Stable IgG Formulation Containing Amino Acids and Trehalose During Freeze-Drying and After Storage: a Central Composite Design.

AAPS PharmSciTech 2019 Mar 27;20(4):154. Epub 2019 Mar 27.

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

The physical and structural stability of freeze-dried immunoglobulin G (IgG) were examined by applying trehalose and amino acids (glycine, phenylalanine, and serine). The efficacy of amino acids was statistically compared considering their side-chain characteristics. The amount of amino acids (X) and trehalose (X) was considered as independent variables. Read More

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http://dx.doi.org/10.1208/s12249-019-1322-2DOI Listing

Self-microemulsifying Drug Delivery System for Improved Oral Delivery of Limonene: Preparation, Characterization, in vitro and in vivo Evaluation.

AAPS PharmSciTech 2019 Mar 26;20(4):153. Epub 2019 Mar 26.

Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.

The current investigation aimed at formulating self-microemulsifying drug delivery system (SMEDDS) to ameliorate oral bioavailability of a hydrophobic functional ingredient, limonene. Solubility test, compatibility test, and pseudo-ternary phase diagrams (PTPD) were adopted to screen the optimal compositions of limonene-SMEDDS (L-SMEDDS). The characteristics of this system assessed in vitro, mainly included determination of particle size distribution, observation of morphology via transmission electron microscopy (TEM), testing of drug release in different dissolution media, and evaluation of stability. Read More

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http://dx.doi.org/10.1208/s12249-019-1361-8DOI Listing
March 2019
1 Read
1.776 Impact Factor

Optimization and Evaluation of Beclomethasone Dipropionate Micelles Incorporated into Biocompatible Hydrogel Using a Sub-Chronic Dermatitis Animal Model.

AAPS PharmSciTech 2019 Mar 25;20(4):152. Epub 2019 Mar 25.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El Aini Street, Cairo, 11562, Egypt.

The current study is concerned with the development and characterization of mixed micelles intended for the dermal delivery of beclomethasone dipropionate, which is a topical corticosteroid used in the management of atopic dermatitis. Mixed micelles were prepared using thin-film hydration technique, employing different concentrations of pluronic L121 with either poloxamer P84 or pluronic F127 with different surfactant mixture-to-drug ratios. The prepared formulae were characterized concerning entrapment efficiency, particle size, and zeta potential. Read More

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http://dx.doi.org/10.1208/s12249-019-1355-6DOI Listing

Improved Oral Absorption of Poorly Soluble Curcumin via the Concomitant Use of Borneol.

AAPS PharmSciTech 2019 Mar 22;20(4):150. Epub 2019 Mar 22.

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

In this study, borneol, a natural active compound was applied to improve the bioavailability of curcumin (CUR). In order to increase CUR solubility and dissolution, solid dispersions (SDs) were prepared with the matrix of polyvinylpyrrolidone (PVP) at various ratios by solvent evaporation method. CUR was evidenced to exist as amorphous state in solid dispersion by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Read More

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http://dx.doi.org/10.1208/s12249-019-1364-5DOI Listing

Cocrystal of 5-Fluorouracil: Characterization and Evaluation of Biopharmaceutical Parameters.

AAPS PharmSciTech 2019 Mar 22;20(4):149. Epub 2019 Mar 22.

University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies (CAS), Panjab University, Sector 14, Chandigarh, 160014, India.

To prepare the cocrystals of 5-fluorouracil (5-FU) with GRAS status coformers via a cocrystallization technique with an aim to improve physicochemical properties as well as bioavailability for colon cancer, breast cancer, and prostate cancer. The mechanochemical method was used in the preparations of three crystals of 5-FU with gentisic acid (5-FUGA), 3,4-dihydroxybenzoic acid (5-FUBA), and 4-aminopyridine (5-FUPN). A thermoanalytical and spectroscopic technique was used for their characterization. Read More

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http://dx.doi.org/10.1208/s12249-019-1360-9DOI Listing
March 2019
3 Reads

Utility of Microcrystalline Cellulose for Improving Drug Content Uniformity in Tablet Manufacturing Using Direct Powder Compression.

AAPS PharmSciTech 2019 Mar 22;20(4):151. Epub 2019 Mar 22.

Department of Pharmaceutical Technology, School of Clinical Pharmacy, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan.

Direct powder compression is the simplest tablet manufacturing method. However, segregation occurs when the drug content is low. It is difficult to assure drug content uniformity in these cases. Read More

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http://dx.doi.org/10.1208/s12249-019-1365-4DOI Listing

Performance Characteristics of a Novel Vibration Technique for the Densification of a Powder Bed within a Die of a Rotary Tablet Press - a Proof of Concept.

AAPS PharmSciTech 2019 Mar 20;20(4):148. Epub 2019 Mar 20.

Division of Pharmaceutical Technology, University of Hamburg, Bundesstr. 45, 20146, Hamburg, Germany.

The aim of this study was to investigate the concept of lower punch vibration as a possible approach to densify the powder bed within the die of a rotary tablet press. Therefore, a laboratory vibration equipment was developed to obtain a better understanding of the performance characteristics and effects of a pneumatically generated vibration system on pharmaceutical powders. For this purpose, two widely used pharmaceutical powders, basic magnesium carbonate (Pharmagnesia MC Type F) and microcrystalline cellulose (Ceolus® KG1000), both with different physical properties, were investigated. Read More

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http://dx.doi.org/10.1208/s12249-019-1351-xDOI Listing

Thermally Induced Denaturing Energetics of Human Blood Plasma Albumin by Differential Scanning Calorimetry (DSC) as an Indicator for Breast Cancer Diagnosis in Female Patients.

AAPS PharmSciTech 2019 Mar 18;20(4):146. Epub 2019 Mar 18.

Drug Delivery System Excellent Center, Department of Pharmaceutical Technology, Faculty of Pharmaceutical Science, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand.

Cancerous invasion yields unusual metabolisms providing a significant amount of peptide albuminomes that modulate albumin stability via binding. The study aimed at the investigation of the thermal stability of human plasma albumin with breast cancer of various stages by means of differential scanning calorimetry (DSC). Blood plasma was drawn from 11 female breast cancer patients and 50 healthy volunteers of homogeneous demographics. Read More

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http://dx.doi.org/10.1208/s12249-019-1356-5DOI Listing

Stability and Bioavailability Enhancement of Telmisartan Ternary Solid Dispersions: the Synergistic Effect of Polymers and Drug-Polymer(s) Interactions.

AAPS PharmSciTech 2019 Mar 18;20(4):143. Epub 2019 Mar 18.

Soli Pharma Sci-Tech Co., Ltd, Economic & Technical Development Zone, Hangzhou, People's Republic of China.

The purpose of this study was to investigate the synergistic effect of polymers and drug-polymer(s) interactions on the improved stability and bioavailability of telmisartan (TEL) ternary solid dispersions. As a water-insoluble drug, 40 and 160 mg doses of TEL tablets exhibited bioavailabilities of 42% and 58%, respectively. Through polymer screening, PVP K30 and/or Soluplus were selected and used at different concentrations to prepare TEL amorphous solid dispersions by solvent evaporation. Read More

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http://dx.doi.org/10.1208/s12249-019-1358-3DOI Listing
March 2019
2 Reads

Highly Soluble Glimepiride and Irbesartan Co-amorphous Formulation with Potential Application in Combination Therapy.

AAPS PharmSciTech 2019 Mar 18;20(4):144. Epub 2019 Mar 18.

School of Engineering and Science, Tecnologico de Monterrey, Campus Monterrey, Ave. Eugenio Garza Sada 2501 Sur., C.P. 64849, Monterrey, N.L., Mexico.

One-third of the population of the USA suffers from metabolic syndrome (MetS). Treatment of patients with MetS regularly includes drugs prescribed simultaneously to treat diabetes and cardiovascular diseases. Therefore, the development of novel multidrug formulations is recommended. Read More

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http://link.springer.com/10.1208/s12249-019-1359-2
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http://dx.doi.org/10.1208/s12249-019-1359-2DOI Listing
March 2019
4 Reads

A Thermoelectric Device for Coupling Fluid Temperature Regulation During Continuous Skin Sonoporation or Sonophoresis.

AAPS PharmSciTech 2019 Mar 18;20(4):147. Epub 2019 Mar 18.

Mechanical Engineering Department, University of Canterbury, Christchurch, New Zealand.

During skin sonoporation and sonophoresis, time-consuming duty cycles or fluid replacement is often required to mitigate coupling fluid temperature increases. This study demonstrates an alternative method for temperature regulation: a circulating, thermoelectric system. Porcine skin samples were sonoporated continuously for 10 min at one of three intensities (23. Read More

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http://dx.doi.org/10.1208/s12249-019-1357-4DOI Listing

Preparation, Characterization, and In vitro Evaluation of Curcumin- and Resveratrol-Loaded Solid Lipid Nanoparticles.

AAPS PharmSciTech 2019 Mar 18;20(4):145. Epub 2019 Mar 18.

Department of Pharmacy Sciences, School of Pharmacy and Health Professions, Creighton University, Omaha, Nebraska, USA.

Curcumin and resveratrol are natural compounds with significant anticancer activity; however, their bioavailability is limited due to poor solubility. This study aimed to overcome the solubility problem by means of solid lipid nanoparticles (SLN). 2-Hydroxypropyl β-cyclodextrin (HPβCD) was selected from a range of polymers based on miscibility and molecular interactions. Read More

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http://dx.doi.org/10.1208/s12249-019-1349-4DOI Listing

Release Adjustment of Two Drugs with Different Solubility Combined in a Matrix Tablet.

AAPS PharmSciTech 2019 Mar 14;20(4):142. Epub 2019 Mar 14.

College of Pharmacy, Freie Universität Berlin, Kelchstrasse 31, 12169, Berlin, Germany.

The objective of this study was to modify the release of two drugs having different solubility in a combined matrix tablet as a fixed-dose combination for extended release. Propranolol HCl (freely soluble) and carbamazepine (very slightly soluble) were used as model drugs, water-soluble hydroxypropyl methylcellulose (HPMC) and water-insoluble ethylcellulose (EC) were used as matrix-forming polymers. Tablets were prepared by direct compression of powder blends, or propranolol HCl was first granulated with one of the matrix-forming polymers (1:1) followed by compression with carbamazepine and matrix former. Read More

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http://link.springer.com/10.1208/s12249-019-1294-2
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http://dx.doi.org/10.1208/s12249-019-1294-2DOI Listing
March 2019
4 Reads

Development and Characterization of Microstructured, Spray-Dried Co-Amorphous Mixture of Antidiabetic Agents Stabilized by Silicate.

AAPS PharmSciTech 2019 Mar 13;20(3):141. Epub 2019 Mar 13.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra, 400056, India.

In the present work, co-amorphous mixture (COAM) of poorly soluble nateglinide (NT) and highly soluble Metformin hydrochloride (MT) was prepared by spray drying method to improve the dissolution rate of NT and the processability of COAM. Binary spray-dried COAM of NT and MT (120 mg: 500 mg) was prepared in its clinical dose ratio whereas 20% Neusilin®US2 (NS) was added to prepare non-sticky, free flowing ternary COAM. Solubility studies of binary and ternary COAM exhibited sevenfold and tenfold rise in the solubility of NT. Read More

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http://link.springer.com/10.1208/s12249-019-1352-9
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http://dx.doi.org/10.1208/s12249-019-1352-9DOI Listing
March 2019
13 Reads

Formulation of Cinnarizine for Stabilization of Its Physiologically Generated Supersaturation.

AAPS PharmSciTech 2019 Mar 11;20(3):139. Epub 2019 Mar 11.

Drug Applied Research Center and School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, 51664, Iran.

Physiologically generated supersaturation and subsequent crystallization of a weakly basic drug in the small intestine leads to compromised bioavailability. In this study, the pH-induced crystallization of cinnarizine (CNZ) in the presence of different polymers was investigated. Inhibitory effect of Eudragit L100 (Eu) on crystallization of CNZ at varying supersaturation ratios was examined. Read More

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http://link.springer.com/10.1208/s12249-019-1338-7
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http://dx.doi.org/10.1208/s12249-019-1338-7DOI Listing
March 2019
2 Reads

Application of the Modified Tangential Spray-Fluidized Bed to Produce Nonpareils from Primary Crystals.

AAPS PharmSciTech 2019 Mar 11;20(3):138. Epub 2019 Mar 11.

GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore, 117543, Singapore.

Coating of fine primary drug particles by a fluidized bed processor has been reported to be potentially challenging. This work aimed to develop a spray layering process to produce nonpareils by a side spray fluid bed with swirling air flow. The first part examined the effects of various parameters for producing lactose nonpareils by using Box-Behnken design. Read More

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http://link.springer.com/10.1208/s12249-019-1345-8
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http://dx.doi.org/10.1208/s12249-019-1345-8DOI Listing
March 2019
2 Reads
1.776 Impact Factor

Pharmaceutical "New Prior Knowledge": Twenty-First Century Assurance of Therapeutic Equivalence.

AAPS PharmSciTech 2019 Mar 12;20(3):140. Epub 2019 Mar 12.

Arnold and Marie Schwartz College of Pharmacy and Health Sciences, 75 DeKalb Avenue, Room WL 313, Brooklyn, New York, 11201, USA.

Facilitating utility of prior knowledge to accelerate evidence-based new drug development is a focus of several communities of knowledge, such as clinical pharmacology. For example, progress has been made via modeling and simulation of pharmacokinetic and pharmacodynamic relationships in the more effective use of "End of Phase 2" regulatory meetings for a New Drug Application (NDA). Facilitating utility of prior "Chemistry, Manufacturing, and Controls" (CMC) knowledge to accelerate new drug development and regulatory review process is also a topic of significant interest. Read More

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http://dx.doi.org/10.1208/s12249-019-1347-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6439171PMC
March 2019
3 Reads

Design of Inhalable Solid Dosage Forms of Budesonide and Theophylline for Pulmonary Combination Therapy.

AAPS PharmSciTech 2019 Mar 7;20(3):137. Epub 2019 Mar 7.

Department of Pharmacy, Faculty of Health and Medical Science, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark.

Corticosteroid resistance poses a major challenge to effective treatment of chronic obstructive pulmonary diseases. However, corticosteroid resistance can be overcome by co-administration of theophylline. The aim of this study was to formulate the corticosteroid budesonide with theophylline into inhalable dry powders intended for pulmonary combination therapy. Read More

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http://dx.doi.org/10.1208/s12249-019-1344-9DOI Listing
March 2019
27 Reads

Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC).

AAPS PharmSciTech 2019 Mar 5;20(3):136. Epub 2019 Mar 5.

School of Pharmacy, The University of Nottingham, Malaysia, Broga Road, Semenyih, Selangor, 43500, Malaysia.

Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6. Read More

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http://dx.doi.org/10.1208/s12249-019-1346-7DOI Listing
March 2019
1.776 Impact Factor

Erlotinib-Valproic Acid Liquisolid Formulation: Evaluating Oral Bioavailability and Cytotoxicity in Erlotinib-Resistant Non-small Cell Lung Cancer Cells.

AAPS PharmSciTech 2019 Mar 4;20(3):135. Epub 2019 Mar 4.

College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, Florida, 32307, USA.

Lung cancer patients develop acquired resistance to tyrosine kinase inhibitors including erlotinib (ERL) after few months of primary treatment. Evidently, new chemotherapy strategies to delay or overcome the resistance are urgently needed to improve the clinical outcome in non-small cell lung cancer (NSCLC) patients. In this paper, we have investigated the cytotoxic interaction of ERL and valproic acid (VA) in ERL-resistant NSCLC cells and developed a liquisolid formulation of ERL-VA for improving oral bioavailability of ERL. Read More

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http://dx.doi.org/10.1208/s12249-019-1332-0DOI Listing
March 2019
4 Reads

Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Animal Studies.

AAPS PharmSciTech 2019 Mar 4;20(3):134. Epub 2019 Mar 4.

Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

Nasal nanovesicular gels of buspirone hydrochloride (BH) were prepared and characterized aiming for sustained delivery and enhancing bioavailability. Buspirone hydrochloride has low bioavailability of about 4% after oral administration due to first pass metabolism. Buspirone hydrochloride nanovesicles were formulated by thin film hydration method (TFH). Read More

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http://dx.doi.org/10.1208/s12249-018-1211-0DOI Listing
March 2019
1 Read

Optimization of Chitosan-α-casein Nanoparticles for Improved Gene Delivery: Characterization, Stability, and Transfection Efficiency.

AAPS PharmSciTech 2019 Feb 28;20(3):132. Epub 2019 Feb 28.

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

Among non-viral vectors, the cationic polymer chitosan has gained attention as a gene delivery system. We hypothesized that the addition of casein into the nanoparticle's structure would facilitate a proper gene transfer. The work herein presented aimed to optimize the production method of chitosan-casein nanoparticles (ChiCas NPs) and to test their ability as a gene delivery system. Read More

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http://dx.doi.org/10.1208/s12249-019-1342-yDOI Listing
February 2019
1 Read

Preparation and Evaluation of Irinotecan Poly(Lactic-co-Glycolic Acid) Nanoparticles for Enhanced Anti-tumor Therapy.

AAPS PharmSciTech 2019 Feb 28;20(3):133. Epub 2019 Feb 28.

The School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Ji'nan, 250012, China.

Irinotecan (IRT), the pro-drug of SN-38, has exhibited potent cytotoxicity against various tumors. In order to enhance the anti-tumor effect of IRT, we prepared IRT-loaded PLGA nanoparticles (IRT-PLGA-NPs) by emulsion-solvent evaporation method. Firstly, IRT-PLGA-NPs were characterized through drug loading (DL), entrapment efficiency (EE), particle size, zeta potential, transmission electron microscopy (TEM), and differential scanning calorimetry (DSC). Read More

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http://link.springer.com/10.1208/s12249-019-1327-x
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http://dx.doi.org/10.1208/s12249-019-1327-xDOI Listing
February 2019
3 Reads
1.776 Impact Factor

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges.

AAPS PharmSciTech 2019 Feb 27;20(3):129. Epub 2019 Feb 27.

Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.

The attempts to oral delivery of lipids can be challenging. Self-emulsifying drug delivery system (SEDDS) plays a vital role to tackle this problem. SEDDS is composed of an oil phase, surfactants, co-surfactants, emulsifying agents, and co-solvents. Read More

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http://link.springer.com/10.1208/s12249-019-1335-x
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http://dx.doi.org/10.1208/s12249-019-1335-xDOI Listing
February 2019
11 Reads

Polyglutamic Acid Functionalization of Chitosan Nanoparticles Enhances the Therapeutic Efficacy of Insulin Following Oral Administration.

AAPS PharmSciTech 2019 Feb 27;20(3):131. Epub 2019 Feb 27.

Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, S.A.S. Nagar, Nagar, Punjab, 160062, India.

In the present study, stable chitosan nanoparticles (Ch-NPs) were developed using the ionotropic gelation method, where poly(sodium 4-styrenesulfonate) (PSS) was used as a cross-linking agent while polyglutamic acid (PGA) for functionalization to improve the oral uptake through calcium-sensing receptors and amino acid transporters present in intestinal epithelium. Formulation was optimized by the design of experiments (DoE) approach using a three-level central composite design and characterized for in vitro parameters such as morphology, particle size, polydispersity index (PDI), entrapment efficiency and zeta potential. Morphological analysis demonstrated the formation of spherical NPs with particle size, zeta potential, and entrapment efficiency in the range of 210 nm ± 2. Read More

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http://dx.doi.org/10.1208/s12249-019-1330-2DOI Listing
February 2019
5 Reads
1.776 Impact Factor

Evaluation of Bio-relevant Mouth-Throat Models for Characterization of Metered Dose Inhalers.

AAPS PharmSciTech 2019 Feb 27;20(3):130. Epub 2019 Feb 27.

Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, Food and Drug Administration, St. Louis, Missouri, 63110, USA.

For inhalation drug characterization, the traditionally used USP induction port provides limited in vivo predictive capability because it does not adequately mimic airway geometry. In this study, various bio-relevant mouth-throat (MT) models, including Alberta Idealized Throat (AIT), and 3D printed large/medium/small-sized VCU (Virginia Commonwealth University) models were evaluated using two metered dose inhaler (MDI) drug products: a solution MDI containing beclomethasone dipropionate (BDP-MDI) and a suspension MDI containing fluticasone propionate (FP-MDI). For BDP-MDI, use of VCU large and small MT models resulted in a significantly higher MT deposition and lower fine particle fraction (FPF) compared with the other MT models. Read More

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http://link.springer.com/10.1208/s12249-019-1339-6
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http://dx.doi.org/10.1208/s12249-019-1339-6DOI Listing
February 2019
12 Reads

The Use of 3D Printed Molds to Cast Tablets with a Designed Disintegration Profile.

AAPS PharmSciTech 2019 Feb 26;20(3):127. Epub 2019 Feb 26.

Group of Manufacturing and Materials, Department of Pharmacy, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark.

Development of new product design principles is crucial for obtaining pharmaceutical products with controlled functionality. Four different molds were designed using a computer-aided design (CAD) software and 3D printed with polylactic acid (PLA). A hydroxypropyl methylcellulose (HPMC) and polyethylene glycol (PEG)-based formulation containing indomethacin as the active pharmaceutical ingredient (API) was casted into the molds. Read More

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http://dx.doi.org/10.1208/s12249-019-1341-zDOI Listing
February 2019
6 Reads

Respiratory Administration of Infliximab Dry Powder for Local Suppression of Inflammation.

AAPS PharmSciTech 2019 Feb 26;20(3):128. Epub 2019 Feb 26.

Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14155-6451, Iran.

The airways are verified as a relevant route to improve antibody therapeutic index with superior lung concentration but limited passage into systemic blood stream. The current research aimed to process spray-dried (SD) powder of Infliximab to assess the feasibility of respiratory delivery of antibody for local suppression of lung-secreted tumor necrosis factor α (TNFα). Molecular and structural stability of powders were determined through size exclusion chromatography (SEC-HPLC) and Fourier transform infrared (FTIR) spectroscopy. Read More

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http://link.springer.com/10.1208/s12249-019-1308-0
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http://dx.doi.org/10.1208/s12249-019-1308-0DOI Listing
February 2019
7 Reads

A Drug Release Model Constructed by Factorial Design to Investigate the Interaction Between Host Mesoporous Silica Carriers and Drug Molecules.

AAPS PharmSciTech 2019 Feb 26;20(3):126. Epub 2019 Feb 26.

Department of Pharmacy, The First Hospital of China Medical University, 155 Nanjing North Street, Shenyang, 110001, Liaoning, China.

A drug release model based on mesocellular foam silica (MCF) for Biopharmaceutics Classification System (BCS) II drugs was conducted. A three-level two-factorial factorial design was carried out for the exploration of the influence of the pore size of MCF (X) and drug-loading degree (X) for drug release behaviors. Cumulative release in 1 h (Y), cumulative release in 24 h (Y), and rate constant k (Y) were selected as dependent response variables. Read More

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http://dx.doi.org/10.1208/s12249-019-1340-0DOI Listing
February 2019
8 Reads

Potential of Lipid Nanoparticles (SLNs and NLCs) in Enhancing Oral Bioavailability of Drugs with Poor Intestinal Permeability.

AAPS PharmSciTech 2019 Feb 25;20(3):121. Epub 2019 Feb 25.

Delhi Pharmaceutical Sciences and Research University (DPSRU), Mehrauli-Badarpur Road, Pusp Vihar Sector 3, New Delhi, 110017, India.

Lipid-based drug delivery systems has become a popular choice for oral delivery of lipophilic drugs with dissolution rate limited oral absorption. Lipids are known to enhance oral bioavailability of poorly water-soluble drugs in multiple ways like facilitating dissolution as micellar solution, enhancing the lymphatic uptake and acting as inhibitors of efflux transporters. Lipid nanoparticles are matrix type lipid-based carrier systems which can effectively encapsulate both lipophilic and hydrophilic drugs. Read More

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http://link.springer.com/10.1208/s12249-019-1337-8
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http://dx.doi.org/10.1208/s12249-019-1337-8DOI Listing
February 2019
8 Reads

Submission of Rifaximin to Different Techniques: Characterization, Solubility Study, and Microbiological Evaluation.

AAPS PharmSciTech 2019 Feb 25;20(3):125. Epub 2019 Feb 25.

Department of Pharmaceutics, School of Pharmaceutical Sciences of Araraquara, Univ Estadual Paulista - UNESP, Araraquara, São Paulo, Brazil.

Rifaximin, an oral antimicrobial drug, is marketed as 200-mg tablets. The daily dose ranges from 600 mg (1 tablet 3 times a day) to 800 mg (2 tablets twice a day). It is used for a wide range of ages, from adults to children, since it is indicated for the treatment of hepatic encephalopathy, travelers' diarrhea, irritable bowel syndrome, Clostridium difficile, ulcerative colitis, and acute diarrhea. Read More

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http://dx.doi.org/10.1208/s12249-019-1329-8DOI Listing
February 2019
6 Reads

Correction to: Enhanced Oral Absorption of Amisulpride Via a Nanostructured Lipid Carrier-Based Capsules: Development, Optimization Applying the Desirability Function Approach and In Vivo Pharmacokinetic Study.

AAPS PharmSciTech 2019 Feb 25;20(3):123. Epub 2019 Feb 25.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El Aini, Cairo, 12411, Egypt.

The second author's name was incorrectly published as "Niha F. Younes". The correct name is "Nihal Farid Younes" as shown above in the list of authors. Read More

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http://dx.doi.org/10.1208/s12249-019-1321-3DOI Listing
February 2019

Effect of pH and Ionic Strength on the Solubility of Quinoline: Back-to-Basics.

AAPS PharmSciTech 2019 Feb 25;20(3):124. Epub 2019 Feb 25.

Department of Pharmacy Practice and Science, College of Pharmacy, University of Arizona, Tucson, Arizona, 85721, USA.

The interest of quinoline as a contaminant agent and as scaffold for the development of new therapeutic agent warrants to revisit the pH-solubility behavior of quinoline (Q) and quinoline derivatives (Q-derivatives) with possible salting-out effect. Q is a weak base with potential hazard upon exposure that may be occupational by inhalation or ingestion of or dermal exposure to particulates in certain industries; or simply by inhalation of cigarette smoke. In contrast, quinoline and its derivatives are useful in diverse therapeutic applications such as anticancer, antiseptic, antipyretic, antiviral, and antimalarial. Read More

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http://link.springer.com/10.1208/s12249-019-1336-9
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http://dx.doi.org/10.1208/s12249-019-1336-9DOI Listing
February 2019
6 Reads

Amphotericin B-Loaded Emulgel: Effect of Chemical Enhancers on the Release Profile and Antileishmanial Activity In Vitro.

AAPS PharmSciTech 2019 Feb 25;20(3):122. Epub 2019 Feb 25.

Federal University of Piauí, Teresina, Piauí, Brazil.

Cutaneous leishmaniasis is a neglected parasitic disease. Treatment is preferably performed with pentavalent antimony associated or not with amphotericin B (AmB). This study aimed to develop an emulgel with different chemical enhancers of cutaneous release. Read More

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http://dx.doi.org/10.1208/s12249-019-1323-1DOI Listing
February 2019
1 Read

Ethambutol-Loaded Solid Lipid Nanoparticles as Dry Powder Inhalable Formulation for Tuberculosis Therapy.

AAPS PharmSciTech 2019 Feb 22;20(3):120. Epub 2019 Feb 22.

Department of Analytical Chemistry, University of Valencia, Dr. Moliner 50, 46100, Burjassot, Valencia, Spain.

Ethambutol hydrocloride (EMB) is an anti-tuberculosis drug, which is commonly used as a protection agent against of unrecognized resistance to other drugs employed to treat this disease. Since oral form of EMB has some side effects and cellular toxicity, direct administration of EMB into lungs seems to be an attractive and reasonable option in order to overcome these side effects. Our main goal in this study was assessment of pulmonary administration through dry powder inhaler (DPI) using EMB-loaded solid lipid nanoparticles (SLNs). Read More

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http://dx.doi.org/10.1208/s12249-019-1334-yDOI Listing
February 2019
4 Reads

pH/Thermo-Dual Responsive Tunable In Situ Cross-Linkable Depot Injectable Hydrogels Based on Poly(N-Isopropylacrylamide)/Carboxymethyl Chitosan with Potential of Controlled Localized and Systemic Drug Delivery.

AAPS PharmSciTech 2019 Feb 21;20(3):119. Epub 2019 Feb 21.

Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur, Punjab, 63100, Pakistan.

In the current study, cytocompatible in situ cross-linkable pH/thermo-dual responsive injectable hydrogels were prepared based on poly(N-isopropylacrylamide) and carboxymethyl chitosan, i.e., poly(CMCS-g-NIPAAm). Read More

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http://dx.doi.org/10.1208/s12249-019-1328-9DOI Listing
February 2019
7 Reads
1.776 Impact Factor