Abstract：
:The clinical potential of naringenin (NRG) is compromised due to its poor aqueous solubility and low oral bioavailability. The study is aimed at addressing these issues by means of naringenin nanosuspensions (NRG-NS) formulated using polyvinylpyrrolidone (PVP K-90) as stabiliser via antisolvent sonoprecipitation method. Optimisation of sonication time, drug concentration and stabilisers was done based on particle size. Characterisation of pure NRG and NRG-NS was carried out by scanning electron microscopy, differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and Fourier transform infrared spectroscopy (FTIR). In vitro dissolution, intestinal absorption by non-everted rat intestinal sac model and in situ single pass intestinal perfusion techniques were performed for further investigation. Nanosuspensions prepared using PVP K-90 lead to minimum particle size (117 ± 5 nm) with zeta potential of -14.6 ± 5.6 mV. The particle size was affected by increasing sonication time, concentration of stabiliser and drug. Nanosizing process converted the crystalline drug into amorphous form as predicted from DSC and XRD patterns. FTIR demonstrated the formation of hydrogen bonds between drug and polymer. NRG-NS displayed a higher dissolution amount (91 ± 4.4% during 60 min) compared to NRG powder (42 ± 0.41%). The apparent and effective permeability of NRG-NS was increased as compared to the pure NRG. The in vivo pharmacokinetics demonstrated that the C max and AUC0-24 h values of NRG-NS were approximately 2- and 1.8-fold superior than the pure drug. Hence, overall results confirmed nanosuspensions as promising approach for NRG delivery with high absorption in gastrointestinal tract, improved dissolution and oral bioavailability.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Gera S,Talluri S,Rangaraj N,Sampathi Sdoi
10.1208/s12249-017-0790-5subject
Has Abstractpub_date
2017-11-01 00:00:00pages
3151-3162issue
8issn
1530-9932pii
10.1208/s12249-017-0790-5journal_volume
18pub_type
杂志文章abstract：:The effects of electron beam or gamma-irradiation on technological performances (capsule hardness, expressed as deforming work and dissolution time) of empty 2-shell capsules made of gelatin or hydroxypropylmethylcellulose (HPMC) were studied. Capsule structural changes induced by radiation treatment were investigated...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt060473
更新日期：2005-12-01 00:00:00
abstract：:Targeted delivery to the lung for controlling lung inflammation is an area that we have explored in this study. The purpose was to use microparticles containing an antisense oligonucleotide (ASO) to NF-κB to inhibit the production of proinflammatory cytokines. Microparticles were prepared using the B-290 Buchi Spray D...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-018-1002-7
更新日期：2018-05-01 00:00:00
abstract：:The addition of polysorbate 20 (T20) is required to achieve "sink" conditions during a dissolution test for tablets with candesartan cilexetil (CC). Polysorbate 20 (0.35%-0.7% w/w) added to 0.05 mol/L of phosphate buffer pH 6.5 dramatically increased the apparent solubility of the drug from 0.8 μg/ml even to 353 μg/ml...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0109-8
更新日期：2014-10-01 00:00:00
abstract：:This study examined the mechanical (hardness, compressibility, adhesiveness, and cohesiveness) and rheological (zero-rate viscosity and thixotropy) properties of polyethylene glycol (PEG) gels that contain different ratios of Carbopol 934P (CP) and polyvinylpyrrolidone K90 (PVP). Mechanical properties were examined us...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt010324
更新日期：2000-08-17 00:00:00
abstract：:A simple but novel mixed surfactant system was designed to fabricate a self-nanoemulsifying drug delivery system (SNEDDS) based on hydrophilic-lipophilic balance (HLB) value. The impacts of HLB and molecular structure of surfactants on the formation of SNEDDS were investigated. After screening various oils and surfact...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0078-y
更新日期：2014-04-01 00:00:00
abstract：:Colorectal cancer is a global concern, and its treatment is fraught with non-selective effects including adverse side effects requiring hospital visits and palliative care. A relatively safe drug formulated in a bioavailability enhancing and targeting delivery platform will be of significance. Metformin-loaded solid l...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0505-3
更新日期：2017-02-01 00:00:00
abstract：:The purpose of this research was to assess the physicochemical properties of a controlled release formulation of recombinant human growth hormone (rHGH) encapsulated in poly(D,L-lactide-co-glycolide) (PLGA) composite microspheres. rHGH was loaded in poly(acryloyl hydroxyethyl) starch (acHES) microparticles, and then t...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040228
更新日期：2003-01-01 00:00:00
abstract：: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 suppres...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1308-0
更新日期：2019-02-26 00:00:00
abstract：:Next to the coating formulation, process conditions play important roles in determining coating quality. This study aims to develop an operational window that separates layering from agglomeration regimes and, furthermore, the one that leads to the best coating quality in a fluidized bed coater. The bed relative humid...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-009-9250-1
更新日期：2009-01-01 00:00:00
abstract：:Hard capsules are made from gelatin, an organic polymer obtained through the hydrolysis of collagen present in animal tissues. Gelatin can be degraded by microorganisms and some strategies can be used to control contaminating micro-organisms. Gamma irradiation is considered as an effective sterilization method; howeve...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1394-z
更新日期：2019-05-20 00:00:00
abstract：:Polymeric films are safe and effective and can be used for vaginal administration of microbicide drug candidates. Dapivirine (DPV), an investigational and clinically advanced antiretroviral drug, was selected as a model compound for this study. We have previously developed and clinically tested a quick-dissolving DPV ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1442-8
更新日期：2019-06-26 00:00:00
abstract：:The objective of the present study is to investigate the confounding effects, if any, of beta-cyclodextrins (βCDs) on corneal permeability coefficients obtained from in vitro transmembrane diffusion studies. Transcorneal permeability studies were carried out with 2-hydroxypropyl-beta-cyclodextrin (HPβCD) and randomly ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0315-z
更新日期：2015-10-01 00:00:00
abstract：:This investigation was undertaken to evaluate practical feasibility of site specific pulmonary delivery of liposomal encapsulated Dapsone (DS) dry powder inhaler for prolonged drug retention in lungs as an effective alternative in prevention of Pneumocystis carinii pneumonia (PCP) associated with immunocompromised pat...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-007-9024-6
更新日期：2008-01-01 00:00:00
abstract：:In this study, we investigated the in vitro characteristics of mefenamic acid (MA) microparticles as well as their effects on DNA damage. MA-loaded chitosan and alginate beads were prepared by the ionotropic gelation process. Microsponges containing MA and Eudragit RS 100 were prepared by quasi-emulsion solvent diffus...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9183-0
更新日期：2009-01-01 00:00:00
abstract：:Pellet manufacturing by extrusion/spheronization is quite common in the pharmaceutical field because the obtained product is characterized by a high sphericity as well as a narrow particle size distribution. The established mechanisms only consider deformation of the initially fractured particles but do not account fo...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9532-7
更新日期：2010-12-01 00:00:00
abstract：:Development of age-appropriate formulation suitable for pediatric and geriatric patients involves various challenges. The objective of this research was to develop extended-release oral flexible tablet (ER-OFT) formulation using carbamazepine (CBZ) as model drug for pediatric and geriatric compliance. ER-microparticle...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0715-3
更新日期：2017-10-01 00:00:00
abstract：:The purpose of this present study was to evaluate the antiangiogenic activity of sterically stabilized liposomes containing paclitaxel (SSL-PTX). The SSL-PTX was prepared by the thin-film method. The release of paclitaxel from SSL-PTX was analyzed using a dialysis method. The effect of SSL-PTX on endothelial cell prol...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9430-z
更新日期：2010-06-01 00:00:00
abstract：:Hypertension remains a significant risk factor for several cardiovascular disorders including coronary artery disease and heart failure. Despite the large armamentarium of drugs available for the management of high blood pressure, low oral availability is an ongoing challenge. Researchers are constantly developing alt...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-019-1583-9
更新日期：2020-01-06 00:00:00
abstract：:Nanotechnology is having a significant impact in the drug delivery systems and diagnostic devices. As most of the nanosystems are intended to be administered in vivo, there is a need for stability models, which could simulate the biological environment. Instability issues could lead to particle aggregation and in turn...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0597-9
更新日期：2017-05-01 00:00:00
abstract：:The aim of the present study was to investigate the use of different grades of microcrystalline cellulose (MCC) and lactose in a direct pelletization process in a rotary processor. For this purpose, a mixed 2- and 3-level factorial study was performed to determine the influence of the particle size of microcrystalline...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt060362
更新日期：2005-10-24 00:00:00
abstract：:A target product profile (TPP) describes how a product will be utilized by the end user. A systematically developed TPP can ensure alignment of objectives across company departments, accelerate development timelines, minimize development risks, and eventually lead to an optimal product. A TPP is particularly important...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-010-9521-x
更新日期：2010-09-01 00:00:00
abstract：:The objective of the present study was to investigate the effects of processing variables and formulation factors on the characteristics of hot-melt extrudates containing a copolymer (Kollidon® VA 64). Nifedipine was used as a model drug in all of the extrudates. Differential scanning calorimetry (DSC) was utilized on...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0226-4
更新日期：2015-04-01 00:00:00
abstract：:The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated as immediate release layer by using various disintegrants like Ac-D...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9116-y
更新日期：2008-01-01 00:00:00
abstract：:Onychomycosis is a chronic disorder that is difficult to manage and hard to eradicate with perilous trends to relapse. Due to increased prevalence of HIV, use of immunosuppressant drugs and lifestyle-related factors, population affected with fungal infection of nail (Onychomycosis) happens to increase extensively in l...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-019-1591-9
更新日期：2020-01-14 00:00:00
abstract：:The aim of the present work was the investigation of robustness and reliability of drug release from 50 to 400 mg quetiapine extended release HPMC matrix tablets towards mechanical stresses of biorelevant intensity. The tests were performed under standard conditions (USP apparatus II) as well as under simulated gastro...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-0050-2
更新日期：2014-02-01 00:00:00
abstract：:Nanoparticles (NPs) containing the hydrophilic drug salidroside (Sal) and the hydrophobic drug tamoxifen (Tam) were prepared using a triblock copolymer poly(lactic-co-glycolic acid) (PLGA)-poly(ethylene glycol) (PEG)-PLGA to achieve synergism in the treatment of breast cancer. The double emulsion (w/o/w) method was us...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1523-8
更新日期：2020-01-29 00:00:00
abstract：:The purpose of this research was to evaluate a new wireless and battery-free sensor technology for invasive product temperature measurement during freeze-drying. Product temperature is the most critical process parameter in a freeze-drying process, in particular during primary drying. The product temperature over time...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9099-8
更新日期：2008-01-01 00:00:00
abstract：:We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0749-6
更新日期：2017-10-01 00:00:00
abstract：:This work describes a quality-by-design (QbD) approach to determine the optimal coating process conditions and robust process operating space for an immediate release aqueous film coating system (Opadry® 200). Critical quality attributes (CQAs) or associated performance indicators of the coated tablets were measured w...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-9935-3
更新日期：2013-06-01 00:00:00
abstract：:Piroxicam is used in the treatment of rheumatoid arthritis, osteoarthritis, and other inflammatory diseases. Upon oral administration, it is reported to cause ulcerative colitis, gastrointestinal irritation, edema and peptic ulcer. Hence, an alternative delivery system has been designed in the form of transethosome. T...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0489-z
更新日期：2017-01-01 00:00:00
