Stimuli-sensitive crosslinked hydrogels as drug delivery systems: Impact of the drug on the responsiveness
Publication date: Available online 17 February 2020Source: International Journal of PharmaceuticsAuthor(s): Carmen Alvarez-Lorenzo, Valerij Y. Grinberg, Tatiana V. Burova, Angel ConcheiroAbstractResponsiveness of drug delivery systems (DDS) against internal and external stimuli attracts wide interest as a mechanism that can provide both site-specific release at the target place and feedback regulated release rate. Biological environment is quite complex and the effects that the intricate medium may have on the effectiveness of the stimulus have received certain attention. Differently, the impact that the drug loaded may ha...
Source: International Journal of Pharmaceutics - February 18, 2020 Category: Drugs & Pharmacology Source Type: research

Human serum albumin nanoparticles as nanovector carriers for proteins: Application to the antibacterial proteins “neutrophil elastase” and “secretory leukocyte protease”
Publication date: Available online 15 February 2020Source: International Journal of PharmaceuticsAuthor(s): Mohamad Tarhini, Anne Pizzoccaro, Ihsane Benlyamani, Chloé Rebaud, Hélène Greige-Gerges, Hatem Fessi, Abdelhamid Elaissari, Abderrazzak BentaherAbstractThe use of proteins and defined amino acid sequences as therapeutic drugs have gained a certain interest in the past decade. However, protein encapsulation within protein nanoparticles was never endeavored. For this reason, human serum albumin (HSA) nanoparticles were prepared by nanoprecipitation method. The process was optimized, and particles w...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Crystallization tendency of APIs possessing different thermal and glass related properties in amorphous solid dispersions
Publication date: Available online 15 February 2020Source: International Journal of PharmaceuticsAuthor(s): Afroditi Kapourani, Elisavet Vardaka, Konstantinos Katopodis, Kyriakos Kachrimanis, Panagiotis BarmpalexisAbstractThe correlation between glass forming ability (GFA) and several thermophysical or physicochemical properties of APIs with the formation and the physical stability of amorphous solid dispersions (ASDs) was evaluated in the present study. Eight poorly water-soluble APIs belonging in different GFA classes (i.e. a) GFA Class I: Carbamazepine, CBZ, b) GFA Class II: Agomelatine, AGO, Aprepitant, APT, Rivaroxaba...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Drug-in-hydroxypropyl-β-cyclodextrin-in-lipoid S100/cholesterol liposomes: effect of the characteristics of essential oil components on their encapsulation and release
In this study, we examined the effect of chemical structure, octanol/water partition coefficient (log P), and Henry’s law constant (Hc) on the encapsulation and the release of monoterpenes (eucalyptol, pulegone, terpineol, and thymol) and phenylpropenes (estragole and isoeugenol) from DCLs. Hydroxypropyl-β-cyclodextrin/EO component (HP-β-CD/EO component) inclusion complexes were prepared in aqueous solution and loaded into liposomes by the ethanol injection method. The phospholipid:cholesterol:EO component molar ratio determined for DCL structures was affected by characteristics of EO components. The presen...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Polyoxazolines Based Lipid Nanocapsules for Topical Delivery of Antioxidants
Publication date: Available online 16 February 2020Source: International Journal of PharmaceuticsAuthor(s): L. Simon, V. Lapinte, L. Lionnard, N. Marcotte, M. Morille, A. Aouacheria, K. Kissa, J.M. Devoisselle, S. BéguAbstractNano-sized lipid formulations offer a great potential for topical delivery of active compounds to treat and prevent human skin damages. Of particular importance is the high loading of hydrophobic molecules, the long-term stability and the auspicious penetration capacity especially reached when using lipid nanocapsules (LNC). Unfortunately, their formation currently relies on a phase inversion p...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Flow-through cell-based In Vitro Release Method for Triamcinolone acetonide Poly (lactic-co-glycolic) acid Microspheres
Publication date: Available online 16 February 2020Source: International Journal of PharmaceuticsAuthor(s): Namita P. Tipnis, Jie Shen, Derek Jackson, Daniel Leblanc, Diane J. BurgessAbstractThe main objective of the current research was to develop a compendial flow-through cell apparatus based in vitro release testing method for sustained-release triamcinolone acetonide–loaded poly (lactic-co-glycolic) acid (PLGA) microspheres. Media-based and instrument-based parameters, such as surfactant type, concentration, media volume, flow rate, and testing temperature, were investigated. In addition, a detailed exploration w...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Enhanced Solid-State Stability of Amorphous Ibrutinib Formulations Prepared by Hot-Melt Extrusion
In this study, HME was applied to solve a real problem in the development of an ibrutinib product, stabilizing the amorphous form. A systematic approach was followed by combining theoretical calculations, high-throughput screening (HTS) focused on physical stability and Principal Components Analysis (PCA). The HTS enabled the evaluation of 33 formulations for physical stability and the PCA was key to select four promising systems. The low relevance of drug loading on the drug crystallization supported the HME tests with a very high drug load of 50%. Milled extrudates were characterized and demonstrated to be fully amorphou...
Source: International Journal of Pharmaceutics - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Nanocarriers as versatile delivery systems for effective management of acne
Publication date: Available online 13 February 2020Source: International Journal of PharmaceuticsAuthor(s): Rinaldo Patel, Priyanka PrabhuAbstractAcne vulgaris is a chronic inflammatory skin disorder affecting mostly females. It has a negative impact on the social life and psychological well-being of the individual. Its pathogenesis involves an exaggerated secretion of sebum, hyperkeratinisation of hair follicles, colonization of anaerobic microbes in the hair follicles, and inflammation. Conventional therapy for acne utilizes antibacterial and anti-inflammatory drugs. Systemic use of these drugs is associated with undesir...
Source: International Journal of Pharmaceutics - February 14, 2020 Category: Drugs & Pharmacology Source Type: research

Glucose-modified carbosilane dendrimers: interaction with model membranes and human serum albumin
In conclusion, our results suggest that the flexibility of a DDM molecule, as well as its typical structure (hydrophobic interior and hydrophilic surface) along with the formation of larger aggregates of DDM2-3Glu, significantly affect the type and extent of interaction with biological structures.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 13, 2020 Category: Drugs & Pharmacology Source Type: research

Switch of tablet manufacturing from high shear granulation to twin-screw granulation using quality by design approach
This study aimed to transfer a high shear granulation (HSG) process to a twin-screw granulation (TSG) process while maintaining equivalent dissolution profiles. Ibuprofen (IBP) was used as poorly soluble model drug. Granules were obtained by HSG or TSG according to a full factorial design. The liquid-to-solid ratio and wet massing time (HSG) or powder throughput (TSG) were selected as factors. The granules were compressed to tablets with immediate release and a drug load of 50% (w/w). Quality attributes (QAs) of the granules, especially the granule strength (GS), and the resulting tablets were evaluated. The effect of proc...
Source: International Journal of Pharmaceutics - February 13, 2020 Category: Drugs & Pharmacology Source Type: research

Applications and delivery mechanisms of hyaluronic acid used for topical/transdermal delivery – A review
Publication date: 30 March 2020Source: International Journal of Pharmaceutics, Volume 578Author(s): Jieyu Zhu, Xudong Tang, Yan Jia, Chi-Tang Ho, Qingrong HuangAbstractThe purpose of this review is to introduce the functionalities of hyaluronic acid (HA) and its potential application as an effective carrier for topical/transdermal delivery. Specifically, several delivery mechanisms of HA were summarized here in order to explain its potential permeation-enhancing roles for the skin, which includes receptor-based delivery pathway, skin hydration, hydrophobic interaction with stratum corneum, bioadhesive properties, and visco...
Source: International Journal of Pharmaceutics - February 13, 2020 Category: Drugs & Pharmacology Source Type: research

Topical delivery of niacinamide: influence of neat solvents
Publication date: Available online 11 February 2020Source: International Journal of PharmaceuticsAuthor(s): Fotis Iliopoulos, Bruno C. Sil, A.S.M. Monjur Al Hossain, David J. Moore, Robert A. Lucas, Majella E. LaneAbstractNiacinamide (NIA) has been widely used in cosmetic and personal care formulations for several skin conditions. Permeation of topical NIA has been confirmed in a number of studies under infinite dose conditions. However, there is limited information in the literature regarding permeation of NIA following application of topical formulations in amounts that reflect the real-life use of such products by consu...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Impact of Product Design Parameters on In Vitro Release from Intrauterine Systems
In this study, ten qualitatively (Q1) and quantitatively (Q2) equivalent LNG-IUSs were manufactured with differences in source (supplier) and dimensions (i.e., thickness) of the outer membrane, drug particle size, dimensions of the drug reservoir (i.e., inner diameter), as well as configuration of the entire IUS. A real-time in vitro release testing method was developed for the LNG-IUSs. In addition, an accelerated release testing method was developed using hydro-alcoholic media in order to reduce the time associated with formulation design. Source variations and thickness of their outer membranes had a great impact on the...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Experimental Design in Formulation Optimization of Vitamin K1 oxide-loaded Nanoliposomes for Skin Delivery
The objective of this study was to formulate VKO in nanoliposomes by using Box–Behnken experimental design to obtain an optimized formula with higher efficiency. The ratio of phospholipid to cholesterol (PC/CHO ratio), VKO concentration and sonication time in low, medium, and high levels were independent variables, while the percent of VKO entrapment efficiency (EE%) and vesicle size were selected as dependent variables. Optimum desirability was identified and an optimized formulation was prepared, characterized, and selected for in vitro VKO release and ex vivo skin permeation. The PC/CHO ratio showed the greatest e...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Drug recrystallization in drug-in-adhesive transdermal delivery system: A case study of deteriorating the mechanical and rheological characteristics of testosterone TDS
In conclusion, this study demonstrated that the extent of drug recrystallization can be quantitatively correlated with the deterioration of performance characteristics of TDS products.Graphical abstractEffect of drug crystallization in TDS on peel adhesion (A); rheology of the adhesive matrix (B); and drug permeation through human cadaver skin samples (C). In Figure B, the relative standard deviations did not exceed 5% of the plotted yield stress values. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Nanocomplexes based polyvinylpyrrolidone K-17PF for ocular drug delivery of naringenin
This study assumes that these PVP medicine complexes can improve ocular permeation and strengthen the drugs’ therapeutic effects. PVP K-17PF (17PF) and naringenin (NAR) could formulate into self-assembly nanocomplexes (17PF-NAR). The optimal formulation featured a 17PF/NAR weight ratio 20:1 with a complexation efficiency of 98.51 ± 0.86 percent, a mean diameter 6.73 ± 0.42 nm, and a polydispersity index 0.254 ± 0.019. This 17PF-NAR nanocomplex ophthalmic solution was stable in well storage at both 4° and 25°C for 12 weeks. The 17PF-NAR nanocomplexes were observed to significantly improve ...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Multicomponent Granular Mixing in a Bohle Bin Blender-Experiments and Simulation
This study investigates a numerical model-based approach to study the effect of the critical process parameters on the mixing dynamics in Bohle bin blender for a moderately cohesive pharmaceutical formulation. The DEM model can be used to provide crucial insights to developed optimized mixing protocols to ascertain the best mixing conditions for different formulation. As for example, as we try to develop a mixing protocol for another formulation with different operational parameters such as loading pattern, rotational speed, and fill percentage, one can device an optimized mixing protocol of the formulation with the help o...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Preparation and evaluation of self-microemulsifying delivery system containing 5-demethyltangeretin on inhibiting xenograft tumor growth in mice
In this study, we aimed to develop and characterize an optimal self-microemulsifying delivery system (SMEDS) formulated for 5-DTAN and to assess its anticancer activity in a xenograft model. SMEDS is a lipid-based formulation and typically comprises oil, surfactant, and co-surfactant. The results from our solubility and compatibility test revealed that ethyl oleate and d-limonene were appropriate for use as an oil phases. The optimal formulation comprised ethyl oleate / d-limonene (10% / 5%), Cremophor® EL (59.5%), and PEG 400 (25.5%). With this optimal formulation, the mean particle size was 97.1 ± 6.50 nm with...
Source: International Journal of Pharmaceutics - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Development and in vitro evaluation of a new adjuvant system containing Salmonella Typhi porins and chitosan
In this study, we have combined Salmonella Typhi porins and chitosan to develop a new adjuvant system to enhance the immunogenicity of the highly purified antigens. Cationic gels, microparticle (1.69±0.01μm) and nanoparticles (337.7±1.7 nm) based on chitosan were prepared with high loading efficiency of porins. Cellular uptake was examined by confocal laser scanning microscopy, and the macrophage activation was investigated by measuring the surface marker as well as the cytokine release in vitro in J774A.1 macrophage murine cells. Porins alone were not taken up by the macrophage cells whereas in combinatio...
Source: International Journal of Pharmaceutics - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

Nasal timosaponin BII dually sensitive in situ hydrogels for the prevention of Alzheimer’s disease induced by lipopolysaccharides
Publication date: Available online 8 February 2020Source: International Journal of PharmaceuticsAuthor(s): Wenyuan Chen, Ruiteng Li, Siqing Zhu, Jinqiu Ma, Lulu Pang, Baiping Ma, Lina Du, Yiguang JinAbstractAlzheimer’s disease (AD) is a common and severe brain disease with a high mortality among the elders, but no highly efficient medications are currently available. For example, timosaponin BII, an efficient anti-AD agent, has low oral bioavailability. Here, timosaponin BII was formulated in a temperature/ion-sensitive in situ hydrogel (ISG) that was well transformed into gels in the nasal environment. Timosaponin B...
Source: International Journal of Pharmaceutics - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

The effect of rotation speed and particle size distribution variability on mixability: An avalanche rheological and multivariate image analytical approach
In conclusion, this study contributes to process understanding and ideas for designing robust mixing operations. It showcases the usefulness of a quantitative visual approach, exemplified by the ARVM, to evaluate material variability and uncover its mechanistic impact on processing.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

Preparation and optimization of fisetin loaded glycerol based soft nanovesicles by Box-Behnken Design
Publication date: Available online 6 February 2020Source: International Journal of PharmaceuticsAuthor(s): Thasleem Moolakkadath, Mohd. Aqil, Abdul Ahad, Syed Sarim Imam, interpreting the data, Arshiya Praveen, Yasmin Sultana, Mohd MujeebAbstractThe present study focused on the development and optimization of glycerosomes for dermal delivery of fisetin. The fisetin loaded glycerosomes formulation was optimized by Box-Behnken design. The independent variables were the lipoid S 100, glycerol, and sonication time, whereas the dependent variables were the vesicles size, entrapment efficiency, and flux. The mechanism of skin pe...
Source: International Journal of Pharmaceutics - February 7, 2020 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “A bioavailability study on microbeads and nanoliposomes fabricated by dense carbon dioxide technologies using human-primary monocytes and flow cytometry assay” [Int. J. Pharm. 570 (2019) 118686]
Publication date: Available online 6 February 2020Source: International Journal of PharmaceuticsAuthor(s): E. Ciaglia, F. Montella, P. Trucillo, M.C. Ciardulli, P. Di Pietro, G. Amodio, P. Remondelli, C. Vecchione, E. Reverchon, N. Maffulli, A.A. Puca, G. Della Porta (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 7, 2020 Category: Drugs & Pharmacology Source Type: research

Applications and Delivery Mechanisms of Hyaluronic Acid used for Topical/Transdermal Delivery - A review
Publication date: Available online 6 February 2020Source: International Journal of PharmaceuticsAuthor(s): Jieyu Zhu, Xudong Tang, Yan Jia, Chi-Tang Ho, Qingrong HuangAbstractThe purpose of this review is to introduce the functionalities of hyaluronic acid (HA) and its potential application as an effective carrier for topical/transdermal delivery. Specifically, several delivery mechanisms of HA were summarized here in order to explain its potential permeation-enhancing roles for the skin, which includes receptor-based delivery pathway, skin hydration, hydrophobic interaction with stratum corneum, bioadhesive properties, an...
Source: International Journal of Pharmaceutics - February 7, 2020 Category: Drugs & Pharmacology Source Type: research

Development of an oral bentonite-based modified-release freeze-dried powder of vactosertib: Pharmacokinetics and anti-colitis activity in rodent models of ulcerative colitis
In this study, a novel bentonite-based, modified-release, freeze-dried powder of vactosertib was developed and evaluated to determine its potential in the treatment of ulcerative colitis. The formulation released vactosertib slowly and steadily in an in vitro drug release test. The extent of vactosertib released from the formulation was markedly low (18.0%) at pH 1.2 but considerably high (95.6%) at pH 7.4. Compared with vactosertib oral solution, the formulation demonstrated a 52.5% lower mean maximum concentration of vactosertib and three times longer median time to maximum concentration without a significant change in t...
Source: International Journal of Pharmaceutics - February 7, 2020 Category: Drugs & Pharmacology Source Type: research

Etoricoxib-loaded bio-adhesive hybridized polylactic acid-based nanoparticles as an intra-articular injection for the treatment of osteoarthritis
Publication date: 30 March 2020Source: International Journal of Pharmaceutics, Volume 578Author(s): Alaa H. Salama, Abdelfattah A. Abdelkhalek, Nermeen A. ElkasabgyAbstractOsteoarthritis is a major problem in elder people. Etoricoxib-loaded bio-adhesive hybridized nanoparticles were prepared using polylactic acid (PLA) and chitosan hydrochloride (CS-HCl) in presence of Captex®200 as a liquid oil, polyvinyl alcohol (PVA) and Tween®80 as surfactants. The study aimed to present a new intra-articular treatment of osteoarthritis with anti-inflammatory as well as bone rebuilding effects. Hybridized nanoparticles were fab...
Source: International Journal of Pharmaceutics - February 7, 2020 Category: Drugs & Pharmacology Source Type: research

Simplification of Fused Deposition Modeling 3D-Printing Paradigm: Feasibility of 1-step Direct Powder Printing for Immediate Release Dosage Form Production
Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Marina Fanous, Sarah Gold, Silvain Muller, Stefan Hirsch, Joerg Ogorka, Georgios ImanidisAbstractDirect powder three-dimensional (3D)-printing (DPP) of tablets to simplify fused deposition modelling (FDM) was explored. The FDM paradigm involving hot-melt extrusion for making 3D-printable drug-loaded filaments as intermediate products for tablet manufacturing has been gaining attention for the decentralized on-site production of personalized dosage forms. For direct 3D-printing, powder blends were loaded into a cartrid...
Source: International Journal of Pharmaceutics - February 6, 2020 Category: Drugs & Pharmacology Source Type: research

Enhanced penetration and anti-psoriatic efficacy of curcumin by improved smartPearls technology with the addition of glycyrrhizic acid
In conclusion, with the addition of GA, a stable amorphous curcumin topical vehicle fabricated by smartPearls technology without extra dermal matrix is available and facilitates penetration efficacy and anti-psoriatic capacity in imiquimod-induced psoriasiform mice.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 6, 2020 Category: Drugs & Pharmacology Source Type: research

Gelatin nanoparticles for NSAID systemic administration: quality by design and artificial neural networks implementation
Publication date: Available online 4 February 2020Source: International Journal of PharmaceuticsAuthor(s): Antigoni E. Koletti, Efstathia Tsarouchi, Afroditi Kapourani, Konstantinos N. Kontogiannopoulos, Andreana N. Assimopoulou, Panagiotis BarmpalexisAbstractThe present study evaluates the preparation of systemic administrated NSAID gelatin nanoparticles with the aid of quality by design and artificial neural networks (ANNs). Specifically, two different preparation techniques (i.e. nanoprecipitation and two-step desolvation) were implemented for the formulation of diclofenac sodium (DLC) gelatin nanoparticles (GNs). Preli...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Calcium zeolites as intelligent carriers in controlled release of bisphosphonates
Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Mariusz Sandomierski, Monika Zielińska, Adam VoelkelAbstractThis work describes the synthesis of calcium zeolites (type A and X) and their use as drug carriers. This is the first example of using calcium zeolites as intelligent carriers that release drugs under the influence of body fluids. Both zeolites and zeolite / drug systems have been extensively characterized. It has been proven that calcium zeolites can be used as carriers of bisphosphonates (drugs against skeletal system diseases). This is due to the fact th...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Facile Strategy by Hyaluronic Acid Functional Carbon Dot-Doxorubicin Nanoparticles for CD44 Targeted Drug Delivery and Enhanced Breast Cancer Therapy
Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Jianping Li, Man Li, Lifeng Tian, Yue Qiu, Qianwen Yu, Xuhui Wang, Rong Guo, Qin HeAbstractA facile approach was developed to synthesize an innovative hyaluronic acid-modified carbon dot-doxorubicin nanoparticles drug delivery platform. CD44 targeted HA-modified carbon dots (HA-CDs) were synthesized as carrier by one-step hydrothermal treatment within one hour with citric acid and branch-PEI as core carbon source. HA not only functioned as carbon dot component but also as hydrophilic group and targeting ligand of this...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Development of (G3-C12)-mediated camptothecin polymeric prodrug targeting to Galectin-3 receptor against androgen-independent prostate cancer
In this study, we synthesized a novel G3-C12-mediated esterase-sensitive tumor-targeting polymeric prodrug of camptothecin (CPT), P(OEGMA-co-CPT-co-G3-C12), and explored its anticancer activity against androgen-independent prostate cancer in vitro and in vivo. Compared to free CPT, the multifunctional polymeric prodrug demonstrated improved water solubility and stability, higher intracellular uptake, and enhanced cytotoxicity in DU145 cells in vitro. Furthermore, it displayed an improved accumulation in the tumor and an enhanced anticancer activity in vivo. Hence, P(OEGMA-co-CPT-co-G3-C12) could be a promising drug in the ...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Bile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability
In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Roller compaction: Infrared thermography as a PAT for monitoring powder flow from feeding to compaction zone
Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Mingzhe Yu, Chalak Omar, Marcus Weidemann, Alexander Schmidt, James D. Litster, Agba D. SalmanAbstractRoller compaction is a continuous dry granulation process, in which powder is compressed by two counter-rotating rollers. During this process, the powder feeding to the compaction zone has a significant effect on product quality. This work investigates the flow of powder from the feeding zone to the compaction zone using online infrared thermography as Process Analytical Technology (PAT) which is achieved via a specia...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Aggregation of chitosan nanoparticles in cell culture: reasons and resolutions
In this study, we revisited the factors that influence the stability of chitosan (Protasan™ UP CL113) nanoparticles prepared with ionotropic gelation, widely recognized to be prone to aggregation, and proposed a model to overcome the negative influence of aggregation while testing in vitro efficacy. Decrease in pH due to cell proliferation, 37°C cell culture temperature, serum in culture media, and incubation time were considered as factors causing chitosan nanoparticles’ aggregation which deteriorates cell culture assay readouts, increases optical density values and leads to false-positive results. Size an...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Partially hydrolyzed polyvinyl alcohol for fusion-based pharmaceutical formulation processes: evaluation of suitable plasticizers
Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Konstantinos Katopodis, Afroditi Kapourani, Elisavet Vardaka, Anna Karagianni, Christina Chorianopoulou, Konstantinos N. Kontogiannopoulos, Dimitrios N. Bikiaris, Kyriakos Kachrimanis, Panagiotis BarmpalexisAbstractThe present study evaluates the effect of several pharmaceutical plasticizers on the thermo-physical and physicochemical properties of partially hydrolyzed poly(vinyl alcohol) (PVA) used in fusion-based pharmaceutical formulation processes. Specifically, the effect of mannitol (MAN), sorbitol (SOR), sucrose...
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Lactoferrin/Hyaluronic acid double-coated lignosulfonate nanoparticles of quinacrine as a controlled release biodegradable nanomedicine targeting pancreatic cancer
In conclusion, the elaborated nanoparticles could be considered as a promising targeted nanotherapy for treatment of pancreatic cancer with higher efficacy& survival rate and lower organ toxicity.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Use of a Temperature Ramp Approach (TRA) to Design an Optimum and Robust Freeze-drying Process for Pharmaceutical Formulations
In this study, a successful freeze-drying process of two model formulations using the TRA was designed. Verification experiments at the optimum processing conditions showed excellent agreement in both product temperature and sublimation rate with the values obtained using the TRA. Thus, the TRA detailed in this study offers a significant advantage to reduce development time and material and enhance the efficiency and robustness of the resulting freeze-drying process.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 4, 2020 Category: Drugs & Pharmacology Source Type: research

Nanoparticle formulation and in vitro efficacy testing of the mitoNEET ligand NL-1 for drug delivery in a brain endothelial model of ischemic reperfusion-injury
This study lays the preliminary work for potential use of mitoNEET as a target and NL-1 as a therapeutic for the treatment of cerebral ischemia and reperfusion injury.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 4, 2020 Category: Drugs & Pharmacology Source Type: research

Multi-functional chitosan polymeric micelles as oral paclitaxel delivery systems for enhanced bioavailability and anti-tumor efficacy
In this study, we designed a novel chitosan derivative (GA-CS-TPGS copolymer) and constructed paclitaxel micelles (PTX-Micelles) designed to have multiple functions associated with the GA-CS-TPGS copolymer (enhanced bioadhesion, inhibited P-gp efflux and drug metabolism in liver) and the micelles (enhanced solubility and permeability) to enhance the bioavailability and anti-tumor efficacy of PTX. The results showed that the PTX-Micelles system could alter the in vivo pharmacokinetic performance and therapeutic effect of PTX via its predesigned functions. The bioavailability of PTX was enhanced approximately 3.80-fold by th...
Source: International Journal of Pharmaceutics - February 3, 2020 Category: Drugs & Pharmacology Source Type: research

Nanopharmaceuticals: A focus on their clinical translatability
Publication date: Available online 1 February 2020Source: International Journal of PharmaceuticsAuthor(s): Sofia Bisso, Jean-Christophe LerouxAbstractNanoscale materials have contributed changing the way biomedical researchers address the biological and therapeutic limitations of conventional drugs and diagnostic agents. Thanks to a plethora of different materials and synthetic routes, particulate carriers can be designed to modify the half-life of compounds, alter their biodistribution and control the drug release profile, eventually providing an overall clinical benefit to patients. While around 50 nanoformulations (excl...
Source: International Journal of Pharmaceutics - February 3, 2020 Category: Drugs & Pharmacology Source Type: research

Selenium-deposited tripterine phytosomes ameliorate the antiarthritic efficacy of the phytomedicine via a synergistic sensitization
This study was devoted to develop nanomedicine containing Tri and Se used for fighting against arthritis via a coordination mechanism. Se-deposited Tri phytosomes (Se@Tri-PTs) were prepared by a melting-hydration/in situ reduction technique and characterized by particle size, ζ potential, morphology, and entrapment efficiency (EE). The resultant Se@Tri-PTs were 126 nm around in particle size with an EE of 98.85%. Se@Tri-PTs exhibited a sustained drug release both in 0.1 M HCl and pH 6.8 PBS compared with Se-free phytosomes (Tri-PTs). The in vivo antiarthritic test demonstrated that Se@Tri-PTs could result in significa...
Source: International Journal of Pharmaceutics - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Synthesis of multimodal polymersomes for targeted drug delivery and MR/fluorescence imaging in metastatic breast cancer model
The objective of the current study is to design and delivery of targeted PEG-PCL nanopolymersomes encapsulated with Gadolinium based Quantum Dots (QDs) and Doxorubicin (DOX) as magnetic resonance-florescence imaging and anti-cancer agent. Diagnostic and therapeutic efficiency of the prepared theranostic formulation was evaluated in vitro and in vivo.Hydrophobic QDs based on indium-copper-gadolinium-zinc sulfide were synthesized and characterized extensively. Hydrophobic QDs and hydrophilic DOX were loaded in PEG-PCL polymersomes through double emulsion method. Drug release pattern was studied in both citrate (pH 5.4) and p...
Source: International Journal of Pharmaceutics - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Fabrication of nanopatterned PLGA films of Curcumin and TPGS for skin cancer
Publication date: Available online 31 January 2020Source: International Journal of PharmaceuticsAuthor(s): S. Malathi, P.S. Pavithra, S. Sridevi, Rama S. VermaAbstractSquamous cell carcinoma treatment has limited therapeutic options and the incidence rate is increasing recently. In the present investigation, we developed poly(lactic-co-glycolic acid) (PLGA) nanopatterned films (NPFs) through poly dimethyl siloxane (PDMS) cast molding technique and explored its therapeutic efficacy in combination with curcumin and tocopherol poly (ethylene glycol) 1000 succinate (TPGS). Herein, we demonstrate the preparation and characteriz...
Source: International Journal of Pharmaceutics - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Physicochemical characterization and pharmacokinetic evaluation of rosuvastatin calcium incorporated solid lipid nanoparticles
Publication date: Available online 31 January 2020Source: International Journal of PharmaceuticsAuthor(s): Fawaz N.S. Al-Heibshy, Ebru Başaran, Rana Arslan, Naile Öztürk, Kevser Erol, Müzeyyen DemirelAbstractRosuvastatin calcium (RCa) is a very efficient antihyperlipidemic agent, however, being a BCS class II drug, results in poor oral bioavailability. The present study focused on the enhancement of oral bioavailability of RCa with solid lipid nanoparticles (SLNs). Physicochemical properties of the particles were evaluated by particle size (PS), polidispersity index (PDI), zeta potential (ZP), DSC, FT-IR, X...
Source: International Journal of Pharmaceutics - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Controlled In Vitro Delivery of Voriconazole and Diclofenac to the Cornea using Contact Lenses for the Treatment of Acanthamoeba Keratitis
Publication date: Available online 31 January 2020Source: International Journal of PharmaceuticsAuthor(s): Siân R. Morgan, Nicole Pilia, Melissa Hewitt, Rachael L. Moses, Ryan Moseley, Philip N. Lewis, Peter W.J. Morrison, Steven L. Kelly, Josie E. Parker, David Whitaker, Andrew J. Quantock, Charles M. HeardAbstractAcanthamoeba keratitis is caused by a protozoal infection of the cornea, with 80% of cases involving the improper use of contact lenses. The infection causes intense pain and is potentially blinding. However, early diagnosis improves treatment efficacy and the chances of healing. Despite the apparent acces...
Source: International Journal of Pharmaceutics - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Mechanistic aspects of drug loading in liquisolid systems with hydrophilic lipid-based mixtures
Publication date: Available online 30 January 2020Source: International Journal of PharmaceuticsAuthor(s): Barbora Vraníková, Andreas Niederquell, Felix Ditzinger, Zdenka Šklubalová, Martin KuentzAbstractDespite the increasing interest in pharmaceutical use of mesoporous silica, there is still only limited knowledge on mechanisms of pore loading and subsequent drug desorption and release. Hence the aim of this work was to address the mechanistic aspects of drug loading into the mesoporous silica pores and to minimise the risk of pore clogging. Hydrophilic solvents (polysorbate 20 and polyethylen...
Source: International Journal of Pharmaceutics - January 31, 2020 Category: Drugs & Pharmacology Source Type: research

A novel, quorum sensor-infused liposomal drug delivery system suppresses Candida albicans biofilms
This study aims to improve the efficacy of a widely used azole, fluconazole by co-delivering it with a Pseudomonas aeruginosa quorum sensing molecule (QSM), N-3-oxo-dodecanoyl-L-homoserine lactone (C12AHL) in a liposomal formulation. C12AHL is known to inhibit C. albicans’ morphological transition and biofilm formation. Four different formulations of liposomes with fluconazole (L-F), with C12AHL (L-H), with fluconazole and C12AHL (L-HF), and a drug-free control (L-C) were prepared using a thin-film hydration followed by extrusion method, and characterised. The effect of liposomes on colonising (90min-24h) and preform...
Source: International Journal of Pharmaceutics - January 31, 2020 Category: Drugs & Pharmacology Source Type: research

Cosm-nutraceutical nanovesicles for acne treatment: Physicochemical characterization and exploratory clinical experimentation
Publication date: Available online 28 January 2020Source: International Journal of PharmaceuticsAuthor(s): Sandra Sherif Amer, Maha Nasr, Rasha T.A. Abdel-Aziz, Noha H. Moftah, Amr El Shaer, Elena Polycarpou, Wael Mamdouh, Omaima SammourAbstractThe full exploration of the ‘nutraceuticals’ therapeutic potential in cosmetics has been hindered by their poor stratum corneum permeation. Therefore, the aim of the present study was to formulate a nutraceutical; quercetin, in novel vitamin C based nanovesicles (aspasomes), and to explore their beneficial effects in the treatment of acne. Aspasomes were characterized fo...
Source: International Journal of Pharmaceutics - January 29, 2020 Category: Drugs & Pharmacology Source Type: research

Chitosan oligosaccharide enhances binding of nanostructured lipid carriers to ocular mucins: Effect on ocular disposition
The objective of the study was to assess the effect of enhanced mucoadhesion of a cationic mucoadhesive nanostructured lipid carrier (NLC) on its ocular disposition after topical administration. The NLC was made mucoadhesive by surface coating with chitosan oligosaccharide (COS), a low molecular weight derivate of chitosan which is more suitable for drug delivery applications as compared to the native chitosan. The NLC was characterised by surface evaluating techniques like SANS and XPS for confirming coating of COS over the surface of NLC. In order to assess the effect of COS coating on in vivo ocular mucoadhesion, coumar...
Source: International Journal of Pharmaceutics - January 29, 2020 Category: Drugs & Pharmacology Source Type: research