Diazepam-loaded solid lipid nanoparticles: design and characterization.

Abstract:

:The aim of the present study was to investigate the feasibility of the inclusion of a water-insoluble drug (diazepam, DZ) into solid lipid nanoparticles (SLNs), which offer combined advantages of rapid onset and prolonged release of the drug. This work also describes a new approach to prepare suppositories containing DZ-loaded SLN dispersions, as potential drug carrier for the rectal route. Modified high-shear homogenization and ultrasound techniques were employed to prepare SLNs. The effect of incorporation of different concentrations of Compritol ATO 888 or Imwitor 900K and Poloxamer 188 or Tween 80 was investigated. Results showed that varying the type or concentration of lipid matrix or surfactant had a noticeable influence on the entrapment efficiencies, particle size, and release profiles of prepared SLNs. Differential scanning calorimetry and X-ray diffraction measurements showed that the majority of SLNs possessed less ordered arrangements of crystals than the corresponding bulk lipids, which was favorable for increasing the drug loading capacity. Transmission electron microscopy and laser diffractometry studies revealed that the prepared nanoparticles were round and homogeneous and 60% of the formulations were less than 500 nm. Additionally, SLN formulations showed significant (P < 0.05) prolonged release than DZ solution. The subsequent step encompassed the preparation and evaluation of SLN-based suppositories utilizing SLN formulations that illustrated optimal release profiles. The in vitro release of DZ from the suppositories prepared using DZ-loaded SLN dispersions (equivalent to 2 mg DZ) was significantly (P < 0.05) extended compared to suppositories containing 2 mg DZ free drug.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Abdelbary G,Fahmy RH

doi

10.1208/s12249-009-9197-2

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

211-9

issue

1

issn

1530-9932

journal_volume

10

pub_type

杂志文章
  • Antiproliferative Activity and VEGF Expression Reduction in MCF7 and PC-3 Cancer Cells by Paclitaxel and Imatinib Co-encapsulation in Folate-Targeted Liposomes.

    abstract::Co-encapsulation of anticancer drugs paclitaxel and imatinib in nanocarriers is a promising strategy to optimize cancer treatment. Aiming to combine the cytotoxic and antiangiogenic properties of the drugs, a liposome formulation targeted to folate receptor co-encapsulating paclitaxel and imatinib was designed in this...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0830-1

    authors: Peres-Filho MJ,Dos Santos AP,Nascimento TL,de Ávila RI,Ferreira FS,Valadares MC,Lima EM

    更新日期:2018-01-01 00:00:00

  • Liposomal oxymatrine in hepatic fibrosis treatment: formulation, in vitro and in vivo assessment.

    abstract::The aim was to develop a liposomal oxymatrine conjugating D-alpha tocopheryl polyethylene glycol 1000 succinate (OMT-LIP) for enhanced therapeutics of hepatic fibrosis. OMT-LIP was prepared using the remote loading method. The influences of formulation compositions on the encapsulation efficiency of OMT-LIP were inves...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0086-y

    authors: Zhang S,Wu J,Wang H,Wang T,Jin L,Shu D,Shan W,Xiong S

    更新日期:2014-06-01 00:00:00

  • Nanocarrier-Based Combination Chemotherapy for Resistant Tumor: Development, Characterization, and Ex Vivo Cytotoxicity Assessment.

    abstract::A folic acid-conjugated paclitaxel (PTX)-doxorubicin (DOX)-loaded nanostructured lipid carrier(s) (FA-PTX-DOX NLCs) were prepared by using emulsion-evaporation method and extensively characterized for particle size, polydispersity index, zeta potential, and % entrapment efficiency which were found to be 196 ± 2.5 nm, ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1185-y

    authors: Raikwar S,Vyas S,Sharma R,Mody N,Dubey S,Vyas SP

    更新日期:2018-11-01 00:00:00

  • Process analytical technology: application to particle sizing in spray drying.

    abstract::The purpose of this research was to explore the possibility of employing PAT for particle sizing during spray drying with the use of an in-line and at-line laser diffraction system. Microspheres were made using maltodextrin and modified starch as wall material and size results obtained using PAT compared with those de...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-007-9011-y

    authors: Chan LW,Tan LH,Heng PW

    更新日期:2008-01-01 00:00:00

  • Formulation and optimization of nonionic surfactants emulsified nimesulide-loaded PLGA-based nanoparticles by design of experiments.

    abstract::This investigation aimed to develop nimesulide (NMS)-loaded poly(lactic-co-glycolic acid) (PLGA)-based nanoparticulate formulations as a biodegradable polymeric drug carrier to treat rheumatoid arthritis. Polymeric nanoparticles (NPs) were prepared with two different nonionic surfactants, vitamin E d-α-tocopheryl poly...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-0048-9

    authors: Turk CT,Oz UC,Serim TM,Hascicek C

    更新日期:2014-02-01 00:00:00

  • Development, optimization, and characterization of solid self-nanoemulsifying drug delivery systems of valsartan using porous carriers.

    abstract::The present studies entail formulation development of novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of valsartan with improved oral bioavailability, and evaluation of their in vitro and in vivo performance. Preliminary solubility studies were carried out and pseudoternary phase diagrams were constr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9865-5

    authors: Beg S,Swain S,Singh HP,Patra ChN,Rao ME

    更新日期:2012-12-01 00:00:00

  • Lectin-Conjugated Clarithromycin and Acetohydroxamic Acid-Loaded PLGA Nanoparticles: a Novel Approach for Effective Treatment of H. pylori.

    abstract::Helicobacter pylori infection remains challenging as it mainly colonized beneath the deep gastric mucosa and adheres to epithelial cells of the stomach. Concanavalin-A (Con-A)-conjugated gastro-retentive poly (lactic-co-glycolic acid) (PLGA) nanoparticles of acetohydroxamic acid (AHA) and clarithromycin (CLR) were pre...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-015-0443-5

    authors: Jain SK,Haider T,Kumar A,Jain A

    更新日期:2016-10-01 00:00:00

  • Behavior of freezable bound water in the bacterial cellulose produced by Acetobacter xylinum: an approach using thermoporosimetry.

    abstract::The aim of the study is to examine thermal behavior of water within reticulated structure of bacterial cellulose (BC) films by sub-ambient differential scanning calorimetry (DSC). BC films with different carbon source, either manitol (BC (a)) or glycerol (BC (b)), were produced by Acetobacter xylinum using Hestrin and...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9104-2

    authors: Kaewnopparat S,Sansernluk K,Faroongsarng D

    更新日期:2008-01-01 00:00:00

  • Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin.

    abstract::Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and diss...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0497-z

    authors: Tang P,Wang L,Ma X,Xu K,Xiong X,Liao X,Li H

    更新日期:2017-01-01 00:00:00

  • Eco-Friendly Tadalafil Surfactant-Free Dry Emulsion Tablets (SFDETs) Stabilized by In Situ Self-Assembled Aggregates of Natural Oil and Native Cyclodextrins.

    abstract::The main principles of green chemistry and engineering were extended to pharmaceutical formulations to prepare eco-friendly surfactant-free dry emulsion tablets (SFDETs) devoid of solvents or synthetic surfactants. Surfactant-free emulsions were stabilized by in situ cyclodextrins/sweet almond oil inclusion complexes ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1450-8

    authors: Badr-Eldin SM,Labib GS,Aburahma MH

    更新日期:2019-07-18 00:00:00

  • Porous Core/Dense Shell PLA Microspheres Embedded with High Drug Loading of Bupivacaine Crystals for Injectable Prolonged Release.

    abstract::Objective of the study was to design an injectable microsphere preparation with high drug loading of bupivacaine for prolonged release and local anesthetic. PLA or PLGA was used as the biodegradable matrix material to fabricate microspheres with the o/w emulsification-solvent evaporation method. The characterization o...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01878-8

    authors: Xu J,Bai Y,Li X,Wei Z,Sun L,Yu H,Xu H

    更新日期:2021-01-06 00:00:00

  • A novel method for analyzing thick tablets by near infrared spectroscopy.

    abstract::A near-infrared (NIR) spectroscopic method to determine content uniformity of a large, thick tablet using an approach that could facilitate future validations has been developed. A CT ibuprofen 800-mg tablet weighs about 1150 mg and is about 18.6 mm wide and 7.6 mm thick. The FT NIR spectrometer was optimized for tran...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020311

    authors: Ramirez JL,Bellamy MK,Romañac RJ

    更新日期:2001-07-12 00:00:00

  • Development of Methotrexate and Minocycline Loaded Nanoparticles for the Effective Treatment of Rheumatoid Arthritis.

    abstract::Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation, and bacterial joint/bone infections. In the present work, methotrexate and minocycline-loaded nanoparticles (MMNPs) were developed with an aim to provide relief from inflammation and disease progression/join...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1581-y

    authors: Janakiraman K,Krishnaswami V,Sethuraman V,Natesan S,Rajendran V,Kandasamy R

    更新日期:2019-12-23 00:00:00

  • Rheological characterization of neutral and anionic polysaccharides with reduced mucociliary transport rates.

    abstract::The purpose of this research was to compare the viscoelastic properties of several neutral and anionic polysaccharide polymers with their mucociliary transport rates (MTR) across explants of ciliated bovine tracheal tissue to identify rheologic parameters capable of predicting the extent of reduction in mucociliary tr...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0802032

    authors: Shah AJ,Donovan MD

    更新日期:2007-04-20 00:00:00

  • Intraoral film containing insulin-phospholipid microemulsion: formulation and in vivo hypoglycemic activity study.

    abstract::Non-invasive administration of insulin is expected for better diabetes mellitus therapy. In this report, we developed intraoral preparation for insulin. Insulin was encapsulated into nanocarrier using self-assembly emulsification process. To increase lipophilicity of insulin, it was dispersed in phospholipid resulted ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0258-9

    authors: Rachmawati H,Haryadi BM,Anggadiredja K,Suendo V

    更新日期:2015-06-01 00:00:00

  • Co-Processed Excipients for Dispersible Tablets-Part 2: Patient Acceptability.

    abstract::Palatability and patient acceptability are critical attributes of dispersible tablet formulation. Co-processed excipients could provide improved organoleptic profile due to rational choice of excipients and manufacturing techniques. The aim of this study was to identify the most suitable co-processed excipient to use ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1104-2

    authors: Dziemidowicz K,Lopez FL,Bowles BJ,Edwards AJ,Ernest TB,Orlu M,Tuleu C

    更新日期:2018-08-01 00:00:00

  • Physicochemical and Preclinical Evaluation of a Novel Buccal Measles Vaccine.

    abstract::The aim of this study is to develop an orally disintegrating film (ODF) containing a microparticulate measles vaccine formulation for buccal delivery. The measles vaccine microparticles were made with biocompatible and biodegradable bovine serum albumin (BSA) and processed by spray drying. These vaccine microparticles...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0566-3

    authors: Gala RP,Popescu C,Knipp GT,McCain RR,Ubale RV,Addo R,Bhowmik T,Kulczar CD,D'Souza MJ

    更新日期:2017-02-01 00:00:00

  • Measurement of fluid viscosity at microliter volumes using quartz impedance analysis.

    abstract::The purpose of this work was to measure viscosity of fluids at low microliter volumes by means of quartz crystal impedance analysis. To achieve this, a novel setup was designed that allowed for measurement of viscosity at volumes of 8 to 10 microL. The technique was based on the principle of electromechanical coupling...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050347

    authors: Saluja A,Kalonia DS

    更新日期:2004-08-05 00:00:00

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

    abstract:: ...

    journal_title:AAPS PharmSciTech

    pub_type: 传,历史文章,新闻

    doi:10.1208/s12249-018-1106-0

    authors: Williams ROB 3rd

    更新日期:2018-08-01 00:00:00

  • Estimating Shelf Life Through Tolerance Intervals.

    abstract::This paper is a continuation of the research published by the Stability Shelf Life Working Group as chartered under the Product Quality Research Institute. The Working Group was formed in 2006 and disbanded in late 2019. Following the philosophy presented by the Working Group on how to characterize the stability shelf...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01800-2

    authors: Schwenke J,Quinlan M,Stroup W,Forenzo P

    更新日期:2020-10-20 00:00:00

  • Pore direction in relation to anisotropy of mechanical strength in a cubic starch compact.

    abstract::The purpose of this research was to evaluate the relation between preferential direction of pores and mechanical strength of cubic starch compacts. The preferential pore direction was quantified in SEM images of cross sections of starch compacts using a previously described algorithm for determination of the quotient ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9074-4

    authors: Wu YS,van Vliet LJ,Frijlink HW,Stokroos I,van der Voort Maarschalk K

    更新日期:2008-01-01 00:00:00

  • Development of Orodispersible Films Containing Benzydamine Hydrochloride Using a Modified Solvent Casting Method.

    abstract::The aim of this study was to develop benzydamine hydrochloride-loaded orodispersible films using the modification of a solvent casting method. An innovative approach was developed when the drying process of a small-scale production was used based on a heated inert base for casting the film. During this process, two ty...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1088-y

    authors: Pechová V,Gajdziok J,Muselík J,Vetchý D

    更新日期:2018-08-01 00:00:00

  • Chitosan gels for the vaginal delivery of lactic acid: relevance of formulation parameters to mucoadhesion and release mechanisms.

    abstract::The aim of this work was to assess the effect of formulation parameters of a mucoadhesive vaginal gel based on chitosan and lactic acid, and to highlight its release mechanisms. Two molecular weight chitosans were used to prepare gels with 2 lactic acid concentrations. Both chitosan molecular weight and lactic acid co...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0704104

    authors: Bonferoni MC,Giunchedi P,Scalia S,Rossi S,Sandri G,Caramella C

    更新日期:2006-01-01 00:00:00

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

    abstract::The present study demonstrates a preparative medium-pressure liquid chromatography (MPLC) method for isolation of Morin besides evaluating its efficacy in comparison with its self-nanoemulsifying drug delivery (SNEDD) and nanoemulsion (NE) systems against in-vivo HgCl2-induced lung toxicity in rats. Morin was isolated...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1072-6

    authors: El-Haddad AE,Sheta NM,Boshra SA

    更新日期:2018-07-01 00:00:00

  • Assessment Methodology for Process Validation Lifecycle Stage 3A.

    abstract::The paper introduces evaluation methodologies and associated statistical approaches for process validation lifecycle Stage 3A. The assessment tools proposed can be applied to newly developed and launched small molecule as well as bio-pharma products, where substantial process and product knowledge has been gathered. T...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-016-0641-9

    authors: Sayeed-Desta N,Pazhayattil AB,Collins J,Chen S,Ingram M,Spes J

    更新日期:2017-07-01 00:00:00

  • Solubilization of cyclosporin A.

    abstract::This study investigated the solubilization of cyclosporin A (CsA), a neutral undecapeptide, by cosolvency, micellization, and complexation. Cosolvents (ethanol, propylene glycol, polyethylene glycol, tetrahydrofurfuryl alcohol polyethyleneglycol ether, and glycerin), surfactants (polyoxyethylene sorbitan monooleate [(...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020102

    authors: Ran Y,Zhao L,Xu Q,Yalkowsky SH

    更新日期:2001-01-18 00:00:00

  • Penetration and distribution of thiocolchicoside through human skin: comparison between a commercial foam (Miotens) and a drug solution.

    abstract::Penetration and distribution of thiocolchicoside from a commercially available foam (Miotens 0.25%, w/v) through human excised full-thickness skin were evaluated using two different in vitro apparatus: a Franz diffusion cell and a Saarbruecken penetration model-based cell. In order to evaluate the intrinsic capability...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9162-5

    authors: Aguzzi C,Rossi S,Bagnasco M,Lanata L,Sandri G,Bona F,Ferrari F,Bonferoni MC,Caramella C

    更新日期:2008-01-01 00:00:00

  • Ultra rapidly dissolving repaglinide nanosized crystals prepared via bottom-up and top-down approach: influence of food on pharmacokinetics behavior.

    abstract::The present work was undertaken with the objectives of improving the dissolution velocity, related oral bioavailability, and minimizing the fasted/fed state variability of repaglinide, a poorly water-soluble anti-diabetic active by exploring the principles of nanotechnology. Nanocrystal formulations were prepared by b...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0267-8

    authors: Gadadare R,Mandpe L,Pokharkar V

    更新日期:2015-08-01 00:00:00

  • Development of Oral Flexible Tablet (OFT) Formulation for Pediatric and Geriatric Patients: a Novel Age-Appropriate Formulation Platform.

    abstract::Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs)...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0666-0

    authors: Chandrasekaran P,Kandasamy R

    更新日期:2017-08-01 00:00:00

  • Photodegradation and stabilization of betamethasone-17 valerate in aqueous/organic solvents and topical formulations.

    abstract::The effects of solvent [acetonitrile, methanol, and acetonitrile/water mixture (20:80, v/v)], buffer concentration (phosphate buffer, pH 7.5), ionic strength and commonly employed adjuvants on the photodegradation of betamethasone-17 valerate in cream and gel formulations have been studied on exposure to UV light (300...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9902-4

    authors: Khattak SU,Shaikh D,Ahmad I,Usmanghani K,Sheraz MA,Ahmed S

    更新日期:2013-03-01 00:00:00