Development and Optimization of an Ex Vivo Colloidal Stability Model for Nanoformulations.

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 could affect the release of the drug from the nanosystems and even lead to clogging of the systemic blood circulation leading to life-threatening situation. We have developed an ex vivo colloidal stability model for testing the stability of nanosystems over a period of 48 h, which is the typical residence time of the nanoparticles in vivo. Tissue homogenates of rat spleen, brain, kidney, and liver were stabilized and optimized for the study; additionally, plasma and serum were used for the same. Poly (lactide-co-glycolic acid) nanoparticles were used as model nanosystem, and no significant change was found in the size and polydispersity index of the nanoparticles in the biological solutions. Moreover, no change in morphology was observed after 48 h as observed by TEM microscopy. Hence, the developed model could prevent the failure of the developed nanosystem during clinical and preclinical application by serving as an initial checkpoint to study their interaction with the complex milieu.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Shaikh MV,Kala M,Nivsarkar M

doi

10.1208/s12249-016-0597-9

subject

Has Abstract

pub_date

2017-05-01 00:00:00

pages

1288-1292

issue

4

issn

1530-9932

pii

10.1208/s12249-016-0597-9

journal_volume

18

pub_type

杂志文章
  • Development and application of a process window for achieving high-quality coating in a fluidized bed coating process.

    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

    authors: Laksmana FL,Hartman Kok PJ,Vromans H,Frijlink HW,Van der Voort Maarschalk K

    更新日期:2009-01-01 00:00:00

  • Direct pelletization in a rotary processor controlled by torque measurements. III. Investigation of microcrystalline cellulose and lactose grade.

    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

    authors: Kristensen J

    更新日期:2005-10-24 00:00:00

  • Stability of benzocaine formulated in commercial oral disintegrating tablet platforms.

    abstract::Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degrad...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-0015-5

    authors: Köllmer M,Popescu C,Manda P,Zhou L,Gemeinhart RA

    更新日期:2013-12-01 00:00:00

  • Chemotherapeutic Efficacy Enhancement in P-gp-Overexpressing Cancer Cells by Flavonoid-Loaded Polymeric Micelles.

    abstract::Multidrug resistance is the major problem in cancer treatment nowadays. Compounds from plants are the new targets to solve this problem. Quercetin (QCT), quercetrin (QTR), and rutin (RUT) are potential anticancer flavonoids but their poor water solubility leads to less efficacy. In this study, the polymeric micelles o...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01657-5

    authors: Khonkarn R,Daowtak K,Okonogi S

    更新日期:2020-04-26 00:00:00

  • Percutaneous Delivery of Antihypertensive Agents: Advances and Challenges.

    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

    authors: Ita K,Ashong S

    更新日期:2020-01-06 00:00:00

  • Polymeric micelles of PEG-PE as carriers of all-trans retinoic acid for stability improvement.

    abstract::The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conju...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9749-0

    authors: Wichit A,Tangsumranjit A,Pitaksuteepong T,Waranuch N

    更新日期:2012-03-01 00:00:00

  • Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier.

    abstract::The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0247-z

    authors: Krupa A,Szlęk J,Jany BR,Jachowicz R

    更新日期:2015-06-01 00:00:00

  • Whey protein/polysaccharide-stabilized emulsions: Effect of polymer type and pH on release and topical delivery of salicylic acid.

    abstract::Emulsions are widely used as topical formulations in the pharmaceutical and cosmetic industries. They are thermodynamically unstable and require emulsifiers for stabilization. Studies have indicated that emulsifiers could affect topical delivery of actives, and this study was therefore designed to investigate the effe...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0081-3

    authors: Combrinck J,Otto A,du Plessis J

    更新日期:2014-06-01 00:00:00

  • Development and evaluation of a floating multiparticulate gastroretentive system for modified release of AZT.

    abstract::The aim of this study was to develop and evaluate a floating multiparticulate gastroretentive system for the modified release of zidovudine (AZT). AZT was used as a model drug water-soluble at therapeutic doses. The floating gastroretentive system was obtained by co-precipitation, after solvent diffusion and evaporati...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9627-9

    authors: Yoshida VM,de Oliveira Junior JM,Gonçalves MM,Vila MM,Chaud MV

    更新日期:2011-06-01 00:00:00

  • Simultaneous Evaluation of Dissolution and Permeation of Oral Drug Solid Formulations for Predicting Absorption Rate-Limiting Factors and In Vitro-In Vivo Correlations: Case Study Using a Poorly Soluble Weakly Basic Drug.

    abstract::Combined dissolution and permeation systems are designed to simultaneously assess the dissolution of a pharmaceutical dosage form and the permeation of dissolved drugs therefrom. However, there were still some limitations on predicting the possible absorption rate-limiting steps and improving the in vitro-in vivo corr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1544-3

    authors: Li Z,He X,Tian S,Feng G,Huang C,Xun M,Wu Z,Wang Y

    更新日期:2019-10-24 00:00:00

  • Chronological Delivery of Antihypertensive Drugs in Bilayered Core-in-Cup Buccoadhesive Tablets: In Vitro and In Vivo Evaluation.

    abstract::Hypertension shows circadian blood pressure rhythms (day-night pattern) that urge the delivery of antihypertensive drugs at the right time in the desired levels. Thus, a bilayered core-in-cup buccoadhesive tablet was formulated that immediately releases olmesartan, to give a burst effect, and controls azelnidipine rel...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1575-9

    authors: Rashad AA,Nageeb El-Helaly S,Abd El Rehim RT,El-Gazayerly ON

    更新日期:2019-12-10 00:00:00

  • Application of pharmaceutical QbD for enhancement of the solubility and dissolution of a class II BCS drug using polymeric surfactants and crystallization inhibitors: development of controlled-release tablets.

    abstract::The aim of this study was to apply quality by design (QbD) for pharmaceutical development of felodipine solid mixture (FSM) containing hydrophilic carriers and/or polymeric surfactants, for easier development of controlled-release tablets of felodipine. The material attributes, the process parameters (CPP), and the cr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9646-6

    authors: Basalious EB,El-Sebaie W,El-Gazayerly O

    更新日期:2011-09-01 00:00:00

  • Tunable Properties of Poly-DL-Lactide-Monomethoxypolyethylene Glycol Porous Microparticles for Sustained Release of Polyethylenimine-DNA Polyplexes.

    abstract::Direct pulmonary delivery is a promising step in developing effective gene therapies for respiratory disease. Gene therapies can be used to treat the root cause of diseases, rather than just the symptoms. However, developing effective therapies that do not cause toxicity and that successfully reach the target site at ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1215-9

    authors: Terry TL,Givens BE,Rodgers VGJ,Salem AK

    更新日期:2019-01-02 00:00:00

  • Excipient selection can significantly affect solid-state phase transformation in formulation during wet granulation.

    abstract::Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The influences of formulation design on the optimal dosage forms should be specified. The aim here was to investigate whether excipients with different water sorption behavior aff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt060241

    authors: Airaksinen S,Karjalainen M,Kivikero N,Westermarck S,Shevchenko A,Rantanen J,Yliruusi J

    更新日期:2005-10-06 00:00:00

  • Optimization, in-vitro Release and in-vivo Evaluation of Gliquidone Nanoparticles.

    abstract::The present work embarks upon increasing the dissolution rate and the bioavailability of model anti-diabetic drug, gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. The gliquidone nanoparticles were prepared by using anti-solvent precipitation technique in which, gliquidone solution in ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1577-7

    authors: Mohamed MS,Abdelhafez WA,Zayed G,Samy AM

    更新日期:2019-12-26 00:00:00

  • Optimization of an aqueous tablet-coating process containing carboxymethylated Cassia fistula gum.

    abstract::The present investigation was aimed at developing and optimizing a simple aqueous tablet-coating formulation and its process. 5-Fluorouracil (5-FU) was used to ascertain the relative lipophilic/hydrophilic behavior of the coating system. Optimization was performed by evaluating the adhesive force strength and cohesive...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9763-x

    authors: Rai PR,Tiwary AK,Rana V

    更新日期:2012-06-01 00:00:00

  • Comparative study of propranolol hydrochloride release from matrix tablets with KollidonSR or hydroxy propyl methyl cellulose.

    abstract::The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or KollidonSR at different concentrations was investigated with a view to developing twice daily sustained release dosage form. A hydrophilic matrix-based tablet using different concentrations of HPMC K15M or ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9092-2

    authors: Sahoo J,Murthy PN,Biswal S,Sahoo SK,Mahapatra AK

    更新日期:2008-01-01 00:00:00

  • Development and validation of a discriminating in vitro dissolution method for a poorly soluble drug, olmesartan medoxomil: comparison between commercial tablets.

    abstract::A dissolution test for tablets containing 40 mg of olmesartan medoxomil (OLM) was developed and validated using both LC-UV and UV methods. After evaluation of the sink condition, dissolution medium, and stability of the drug, the method was validated using USP apparatus 2, 50 rpm rotation speed, and 900 ml of deaerate...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9421-0

    authors: Bajerski L,Rossi RC,Dias CL,Bergold AM,Fröehlich PE

    更新日期:2010-06-01 00:00:00

  • Investigation on side-spray fluidized bed granulation with swirling airflow.

    abstract::Top-spray fluidized bed granulation with axial fluidization airflow from the bottom of the granulator is well-established in the pharmaceutical industry. The application of swirling airflow for fluidized bed granulation was more recently introduced. This study examined the effects of various process parameters on the ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9906-0

    authors: Wong PM,Chan LW,Heng PW

    更新日期:2013-03-01 00:00:00

  • Kinetics of pramlintide degradation in aqueous solution as a function of temperature and pH.

    abstract::The stability of the 37-amino acid peptide pramlintide, in aqueous solution, was studied as a function of pH and temperature. Samples of pramlintide formulated as a parenteral product were exposed to elevated temperatures and to realistic storage conditions for as long as 30 months. Pramlintide degradation was monitor...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt010207

    authors: Kenley RA,Tracht S,Stepanenko A,Townsend M,L'Italien J

    更新日期:2000-03-18 00:00:00

  • Direct compression behavior of low- and high-methoxylated pectins.

    abstract::The objective of this study was to evaluate possible usefulness of pectins for direct compression of tablets. The deformation behavior of pectin grades of different degree of methoxylation (DM), namely, 5%, 10%, 25%, 35%, 40%, 50%, and 60% were, examined in terms of yield pressures (YP) derived from Heckel profiles fo...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-009-9349-4

    authors: Salbu L,Bauer-Brandl A,Tho I

    更新日期:2010-03-01 00:00:00

  • The studies of phase equilibria and efficiency assessment for self-emulsifying lipid-based formulations.

    abstract::The study was designed to build up a database for the evaluation of the self-emulsifying lipid formulations performance. A standard assessment method was constructed to evaluate the self-emulsifying efficiency of the formulations based on five parameters including excipients miscibility, spontaneity, dispersibility, h...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9773-8

    authors: Shahba AA,Mohsin K,Alanazi FK

    更新日期:2012-06-01 00:00:00

  • Clinically Relevant In Vitro Testing of Orally Inhaled Products-Bridging the Gap Between the Lab and the Patient.

    abstract::Current pharmacopeial methods for in vitro orally inhaled product (OIP) performance testing were developed primarily to support requirements for drug product registration and quality control. In addition, separate clinical studies are undertaken in order to quantify safety and efficacy in the hands of the patient. How...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-016-0543-x

    authors: Mitchell JP,Suggett J,Nagel M

    更新日期:2016-08-01 00:00:00

  • Use of Risk Assessment and Plackett-Burman Design for Developing Resveratrol Spray-Dried Emulsions: a Quality-by-Design Approach.

    abstract::In this study, the resveratrol spray-dried emulsions were developed using a quality-by-design approach. Further, the product and process factors that affected the quality of the spray-dried emulsions were analyzed and illustrated using an Ishikawa diagram. The product and process risks were prioritized using a risk-ra...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1220-z

    authors: Benjasirimongkol P,Piriyaprasarth S,Moribe K,Sriamornsak P

    更新日期:2018-12-18 00:00:00

  • Effect of Carbopol and polyvinylpyrrolidone on the mechanical, rheological, and release properties of bioadhesive polyethylene glycol gels.

    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

    authors: Tan YT,Peh KK,Al-Hanbali O

    更新日期:2000-08-17 00:00:00

  • Preparation of gelatin microbeads with a narrow size distribution using microchannel emulsification.

    abstract::The purpose of this study was to prepare monodisperse gelatin microcapsules containing an active agent using microchannel (MC) emulsification, a novel technique for preparing water-in-oil (W/O) and oil-in-water (O/W) emulsions. As the first step in applying MC emulsification to the preparation of monodisperse gelatin ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt030325

    authors: Iwamoto S,Nakagawa K,Sugiura S,Nakajima M

    更新日期:2002-01-01 00:00:00

  • Permeation-Enhancing Nanoparticle Formulation to Enable Oral Absorption of Enoxaparin.

    abstract::This study tests the hypothesis that association complexes formed between enoxaparin and cetyltrimethylammonium bromide (CTAB) augment permeation across the gastrointestinal mucosa due to improved encapsulation of this hydrophilic macromolecule within biocompatible poly (lactide-co-glycolide, PLGA RG 503) nanoparticle...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-1618-2

    authors: Eleraky NE,Swarnakar NK,Mohamed DF,Attia MA,Pauletti GM

    更新日期:2020-02-03 00:00:00

  • Formulation and In Vitro Release Kinetics of Mucoadhesive Blend Gels Containing Matrine for Buccal Administration.

    abstract::Enterovirus 71 (EV71) is a pathogenic factor of severe hand, foot, and mouth disease (HFMD). No vaccine or specific treatment is currently available for EV71 infection. Hence, we developed a buccal mucoadhesive gel containing matrine to protect against HFMD. Mucoadhesive gels were prepared by Carbopol 974P and were co...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0853-7

    authors: Chen X,Yan J,Yu S,Wang P

    更新日期:2018-01-01 00:00:00

  • Systematic Development of Transethosomal Gel System of Piroxicam: Formulation Optimization, In Vitro Evaluation, and Ex Vivo Assessment.

    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

    authors: Garg V,Singh H,Bhatia A,Raza K,Singh SK,Singh B,Beg S

    更新日期:2017-01-01 00:00:00

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

    abstract::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 limone...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1361-8

    authors: Zhu Y,Xu W,Zhang J,Liao Y,Firempong CK,Adu-Frimpong M,Deng W,Zhang H,Yu J,Xu X

    更新日期:2019-03-26 00:00:00