Polyhydroxy surfactants for the formulation of lipid nanoparticles (SLN and NLC): effects on size, physical stability and particle matrix structure.

Abstract:

:The two polyhydroxy surfactants polyglycerol 6-distearate (Plurol(®)Stearique WL1009 - (PS)) and caprylyl/capryl glucoside (Plantacare(®) 810 - (PL)) are a class of PEG-free stabilizers, made from renewable resources. They were investigated for stabilization of aqueous solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) dispersions. Production was performed by high pressure homogenization, analysis by photon correlation spectroscopy (PCS), laser diffraction (LD), zeta potential measurements and differential scanning calorimetry (DSC). Particles were made from Cutina CP as solid lipid only (SLN) and its blends with Miglyol 812 (NLC, the blends containing increasing amounts of oil from 20% to 60%). The obtained particle sizes were identical for both surfactants, about 200 nm with polydispersity indices below 0.20 (PCS), and unimodal size distribution (LD). All dispersions with both surfactants were physically stable for 3 months at room temperature, but Plantacare (PL) showing a superior stability. The melting behaviour and crystallinity of bulk lipids/lipid blends were compared to the nanoparticles. Both were lower for the nanoparticles. The crystallinity of dispersions stabilized with PS was higher, the zeta potential decreased with storage time associated with this higher crystallinity, and leading to a few, but negligible larger particles. The lower crystallinity particles stabilized with PL remained unchanged in zeta potential (about -50 mV) and in size. These data show that surfactants have a distinct influence on the particle matrix structure (and related stability and drug loading), to which too little attention was given by now. Despite being from the same surfactant class, the differences on the structure are pronounced. They are attributed to the hydrophobic-lipophilic tail structure with one-point anchoring in the interface (PL), and the loop conformation of PS with two hydrophobic anchor points, i.e. their molecular structure and its interaction with the matrix surface and matrix bulk. Analysis of the effects of the surfactants on the particle matrix structure could potentially be used to further optimization of stability, drug loading and may be drug release.

journal_name

Int J Pharm

authors

Kovacevic A,Savic S,Vuleta G,Müller RH,Keck CM

doi

10.1016/j.ijpharm.2010.12.036

subject

Has Abstract

pub_date

2011-03-15 00:00:00

pages

163-72

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(11)00008-1

journal_volume

406

pub_type

杂志文章
  • Transcutaneous immunisation assisted by low-frequency ultrasound.

    abstract::Low-frequency ultrasound application is known to increase the skin's permeability to large molecules such as vaccines, and to enable transcutaneous immunisation. Sodium dodecyl sulphate (SDS) - a skin irritant - is often included in the coupling medium at 1% (w/v), as this has been found to enhance skin permeability. ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.10.014

    authors: Dahlan A,Alpar HO,Stickings P,Sesardic D,Murdan S

    更新日期:2009-02-23 00:00:00

  • Tumor targeted delivery of octreotide-periplogenin conjugate: Synthesis, in vitro and in vivo evaluation.

    abstract::Periplogenin (PPG), a cardiac glycoside prepared from Cortex periplocae, with similar structure to bufalin, has been found to induce apoptosis in many tumor cells. However, lots of cardiac glycosides possessing strong antitumor activity in vitro have still not passed phase I clinical trials, mostly due to poor tumor s...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.02.024

    authors: Zhang HY,Xu WQ,Wang YW,Omari-Siaw E,Wang Y,Zheng YY,Cao X,Tong SS,Yu JN,Xu XM

    更新日期:2016-04-11 00:00:00

  • Investigation of pluronic and PEG-PE micelles as carriers of meso-tetraphenyl porphine for oral administration.

    abstract::Meso-tetraphenyl porphine (mTPP) is a highly lipophilic, fluorescent porphyrin derivate and it is used as photosensitizer on the treatment of malign neoplasms. The aim of this study was to prepare mTPP loaded pluronic F127 and polyethylene glycol-distearoyl phosphatidylethanolamine (PEG(2000)-DSPE) micelles to evaluat...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.09.030

    authors: Sezgin Z,Yuksel N,Baykara T

    更新日期:2007-03-06 00:00:00

  • Characterization of nifedipine solid dispersions.

    abstract::The sublingual administration of nifedipine (NIF) is currently used in clinical practice. The sublingual administration of NIF solid dispersions (SD), by using a suitable dispenser, appears an interesting approach in the treatment of moderate and severe hypertensive emergencies. With this aim nine SD made of NIF and a...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00173-4

    authors: Cilurzo F,Minghetti P,Casiraghi A,Montanari L

    更新日期:2002-08-21 00:00:00

  • Comparative study of Pluronic(®) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats.

    abstract::Liposomes modified using cationic and hydrophilic nonionic polymers are 2 popular carriers for improving oral drug absorption. Cationic polymer-modified liposomes can adhere to the intestinal wall mucus (mucoadhesive type), while liposomes modified using hydrophilic nonionic polymers can penetrate across the mucus bar...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.04.002

    authors: Chen D,Xia D,Li X,Zhu Q,Yu H,Zhu C,Gan Y

    更新日期:2013-06-05 00:00:00

  • Integrity and stability of oral liposomes containing bile salts studied in simulated and ex vivo gastrointestinal media.

    abstract::The objective of this study was to investigate the integrtity and stability of oral liposomes containing glycocholate (SGC-Lip) in simulated gastrointestinal (GI) media and ex vivo GI media from rats in comparison with conventional liposomes (CH-Lip) composed of soybean phosphatidylcholine and cholesterol. Membrane in...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.10.025

    authors: Hu S,Niu M,Hu F,Lu Y,Qi J,Yin Z,Wu W

    更新日期:2013-01-30 00:00:00

  • Enhanced preclinical efficacy of tamoxifen developed as alginate-cysteine/disulfide bond reduced albumin nanoparticles.

    abstract::Tamoxifen (TMX) is the most common clinical choice for the treatment of advanced or metastatic estrogen-dependent breast cancer. However, research on new challenging therapies is necessary due to its undesirable side effects and the limitation of the treatment only to the oral route. In this study, the antitumor activ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.045

    authors: Martínez A,Muñiz E,Iglesias I,Teijón JM,Blanco MD

    更新日期:2012-10-15 00:00:00

  • Preparation and characterization of a synthetic curcumin analog inclusion complex and preliminary evaluation of in vitro antileishmanial activity.

    abstract::The aim of this work was to prepare and characterize inclusion complexes between a synthetic curcumin analog (dibenzalacetone, DBA) and beta-cyclodextrin (β-CD); and to evaluate their in vitro antileishmanial activity. DBA was synthetized and characterized by spectroscopic methods and the inclusion complexes were obta...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119764

    authors: Pinto LMA,Adeoye O,Thomasi SS,Francisco AP,Carvalheiro MC,Cabral-Marques H

    更新日期:2020-08-25 00:00:00

  • Critical quality attributes, in vitro release and correlated in vitro skin permeation-in vivo tape stripping collective data for demonstrating therapeutic (non)equivalence of topical semisolids: A case study of "ready-to-use" vehicles.

    abstract::This work aimed to prove the ability of "ready-to-use" topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.06.018

    authors: Ilić T,Pantelić I,Lunter D,Đorđević S,Marković B,Ranković D,Daniels R,Savić S

    更新日期:2017-08-07 00:00:00

  • Novel O-palmitoylscleroglucan-coated liposomes as drug carriers: development, characterization and interaction with leuprolide.

    abstract::Polysaccharide-coated liposomes have been studied for their potential use for peptide drug delivery by the oral route because they are able to minimize the disruptive influences on peptide drugs of gastrointestinal fluids. The aim of this work was to synthesize and characterize a modified polysaccharide, O-palmitoylsc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.06.040

    authors: Carafa M,Marianecci C,Annibaldi V,Di Stefano A,Sozio P,Santucci E

    更新日期:2006-11-15 00:00:00

  • Blend uniformity analysis of pharmaceutical products by Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS).

    abstract::Blend uniformity analysis (BUA) is a routine and highly regulated aspect of pharmaceutical production. In most instances, it involves quantitative determination of individual components of a blend in order to ascertain the mixture ratio. This approach often entails the use of costly and sophisticated instrumentation a...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.07.073

    authors: Fitzpatrick D,Scanlon E,Krüse J,Vos B,Evans-Hurson R,Fitzpatrick E,McSweeney S

    更新日期:2012-11-15 00:00:00

  • Sponges carrying self-microemulsifying drug delivery systems.

    abstract::Self-microemulsifying drug delivery systems (SMEDDS) increase the solubility of lipophilic drugs. One barrier to their wide application is their liquid nature. We report on a new method to solidify SMEDDS-their incorporation in sponges made from a hydrophilic natural polymer. Using different freeze-drying schemes, spo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.09.024

    authors: Josef E,Bianco-Peled H

    更新日期:2013-12-15 00:00:00

  • Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application.

    abstract::NLC topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based NLC formulation containing 75% Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100-750 mg)...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.10.004

    authors: Nnamani PO,Hansen S,Windbergs M,Lehr CM

    更新日期:2014-12-30 00:00:00

  • Passive asymmetric transport of hesperetin across isolated rabbit cornea.

    abstract::Hesperetin, an aglycone of the flavanone hesperidin, is a potential candidate for the treatment of diabetic retinopathy and macular edema. The purpose of this investigation was to determine solubility, stability and in vitro permeability characteristics of hesperetin across excised rabbit corneas. Aqueous and pH depen...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.04.036

    authors: Srirangam R,Majumdar S

    更新日期:2010-07-15 00:00:00

  • Activity of vancomycin release from bioinspired coatings of hydroxyapatite or TiO2 nanotubes.

    abstract::Herein we investigate the efficiency of various biomimetic coatings for localized drug delivery, using vancomycin as key therapeutic drug, which is a widely used antibiotic for the treatment of strong infections caused by positive Gram bacteria. We evaluate classical hydroxyapatite and biomimetic hydroxyapatite-collag...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.11.062

    authors: Ionita D,Bajenaru-Georgescu D,Totea G,Mazare A,Schmuki P,Demetrescu I

    更新日期:2017-01-30 00:00:00

  • A micelle-like structure of poloxamer-methotrexate conjugates as nanocarrier for methotrexate delivery.

    abstract::The purpose of this study was to develop a novel featured and flexible methotrexate (MTX) formulation, in which MTX was physically entrapped and chemically conjugated in the same drug delivery system. A series of poloxamer-MTX (p-MTX) conjugates was synthesized, wherein MTX was grafted to poloxamer through an ester bo...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.04.014

    authors: Ren J,Fang Z,Yao L,Dahmani FZ,Yin L,Zhou J,Yao J

    更新日期:2015-06-20 00:00:00

  • Buccal absorption of ergotamine tartrate using the bioadhesive tablet system in guinea-pigs.

    abstract::The buccal administration of ergotamine tartrate (ET) combined with polyvinyl alcohol (PVA) gel brought about higher plasma concentration of ET compared with that of oral administration of capsules in guinea-pigs. T(max) of ET in plasma of buccal administration was significantly smaller than that of oral administratio...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00070-4

    authors: Tsutsumi K,Obata Y,Nagai T,Loftsson T,Takayama K

    更新日期:2002-05-15 00:00:00

  • Design and characterization of submicron formulation for a poorly soluble drug: the effect of Vitamin E TPGS and other solubilizers on skin permeability enhancement.

    abstract::In transdermal drug delivery systems (TDDS), it is a challenge to achieve stable and prolonged high permeation rates across the skin since the concentrations of the drug dissolved in the matrix have to be high in order to maintain zero order release kinetics. Several attempts have been reported to improve the permeabi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.05.031

    authors: Ghosh I,Michniak-Kohn B

    更新日期:2012-09-15 00:00:00

  • Drug-surfactant-propellant interactions in HFA-formulations.

    abstract::The required replacement of chlorofluorocarbon (CFC) with hydrofluoroalkane (HFA) propellants has challenged formulators of pressurized metered dose inhalers in several major respects. Conventional (CFC soluble) surfactants are effectively insoluble in the major CFC replacement candidates, HFA 134 and HFA 227ea, in th...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/s0378-5173(99)00134-9

    authors: Vervaet C,Byron PR

    更新日期:1999-09-10 00:00:00

  • Predicting the solubility-permeability interplay when using cyclodextrins in solubility-enabling formulations: model validation.

    abstract::Although the extraordinary solubility advantage afforded by cyclodextrins has led to their widespread use as pharmaceutical solubilizers, several reports have emerged that cyclodextrins may also reduce the apparent permeability of the drug. With the purpose to investigate this solubility-permeability interplay, we hav...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.03.017

    authors: Miller JM,Dahan A

    更新日期:2012-07-01 00:00:00

  • Dual anticancer drug/superparamagnetic iron oxide-loaded PLGA-based nanoparticles for cancer therapy and magnetic resonance imaging.

    abstract::We developed dual paclitaxel (PTX)/superparamagnetic iron oxide (SPIO)-loaded PLGA-based nanoparticles for a theranostic purpose. Nanoparticles presented a spherical morphology and a size of 240 nm. The PTX and iron loading were 1.84 ± 0.4 and 10.4 ± 1.93 mg/100 mg respectively. Relaxometry studies and phantom MRI dem...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.02.042

    authors: Schleich N,Sibret P,Danhier P,Ucakar B,Laurent S,Muller RN,Jérôme C,Gallez B,Préat V,Danhier F

    更新日期:2013-04-15 00:00:00

  • Effects of permeation enhancers on flufenamic acid delivery in Ex vivo human skin by confocal Raman microscopy.

    abstract::For effective topical delivery, a drug must cross the stratum corneum (SC) barrier into viable tissue. The use of permeation enhancers is a widespread approach for barrier modification. In the current study, flufenamic acid (FluA), a non-steroidal anti-inflammatory drug, is a model agent for investigating the influenc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.04.011

    authors: Pyatski Y,Zhang Q,Mendelsohn R,Flach CR

    更新日期:2016-05-30 00:00:00

  • Effect of process parameters on compressibility of granulation manufactured in a high-shear mixer.

    abstract::Various processing variables that can influence granulation characteristics of a lactose-based formulation were evaluated using a Plackett-Burman experimental design. These parameters were impeller speed, granulating solution addition rate, total amount of water added in the granulation step, wet massing time, moistur...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00445-7

    authors: Badawy SI,Menning MM,Gorko MA,Gilbert DL

    更新日期:2000-03-30 00:00:00

  • Retention and distribution of two 99mTc-DTPA labelled vaginal dosage forms.

    abstract:UNLABELLED:To objectively evaluate the performance of new vaginal dosage forms, it is important to determine their time of residence and their distribution. This paper describes the in vivo characteristics of a reference and test product in this situation. METHOD:A randomised cross-over study was performed in the same...

    journal_title:International journal of pharmaceutics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/j.ijpharm.2003.11.006

    authors: Chatterton BE,Penglis S,Kovacs JC,Presnell B,Hunt B

    更新日期:2004-03-01 00:00:00

  • Localized drug delivery with mono and bilayered mucoadhesive films and wafers for oral mucosal infections.

    abstract::Local drug delivery into oral cavity offers many advantages over systemic administration in treatment of the oral infections. In this study, monolayer and bilayered mucoadhesive film and wafer formulations were developed as local drug delivery platforms using chitosan and hydroxypropyl methylcellulose (HPMC). Cefuroxi...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.01.029

    authors: Timur SS,Yüksel S,Akca G,Şenel S

    更新日期:2019-03-25 00:00:00

  • Preparation of poly(DL-lactide-co-glycolide) nanoparticles by modified spontaneous emulsification solvent diffusion method.

    abstract:PURPOSE:The objectives of this study were to establish a new preparation method for poly(DL-lactide-co-glycolide) (PLGA) nanoparticles by modifying the spontaneous emulsification solvent diffusion (SESD) method and to elucidate the mechanism of nanoparticle formation on the basis of the phase separation principle of PL...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(99)00187-8

    authors: Murakami H,Kobayashi M,Takeuchi H,Kawashima Y

    更新日期:1999-10-05 00:00:00

  • Polyamine metabolism-based dual functional gene delivery system to synergistically inhibit the proliferation of cancer.

    abstract::Polyamine content, which is associated with tumor growth, can be regulated by ornithine decarboxylase (ODC) and S-adenosyl methionine decarboxylase (SAMDC), two key enzymes in polyamine biosynthesis. Here we aim to develop a pH-responsive cationic poly(agmatine) based on a polyamine analogue-agmatine that can dually f...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.04.039

    authors: Cui PF,Xing L,Qiao JB,Zhang JL,He YJ,Zhang M,Lyu JY,Luo CQ,Jin L,Jiang HL

    更新日期:2016-06-15 00:00:00

  • Effects of pretreatment of needle puncture and sandpaper abrasion on the in vitro skin permeation of fluorescein isothiocyanate (FITC)-dextran.

    abstract::Microneedle systems have gained attention as having many advantages over transdermal patches and hypodermic needles. The procedure provides adequate skin permeation rates without pain or severe infection. To obtain information for designing a microneedle system, macroneedles were used instead of microneedles to invest...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.02.046

    authors: Wu XM,Todo H,Sugibayashi K

    更新日期:2006-06-19 00:00:00

  • The influence of high shear mixing on ternary dry powder inhaler formulations.

    abstract::The blending process is a key step in the production of dry powder inhaler formulations, but only little is known about the influence of process parameters. This is especially true for high shear blending of ternary formulations. For this reason, this study aims to investigate the influence of high shear mixing proces...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.10.033

    authors: Hertel M,Schwarz E,Kobler M,Hauptstein S,Steckel H,Scherließ R

    更新日期:2017-12-20 00:00:00

  • Physicochemical characterization techniques for lipid based delivery systems for siRNA.

    abstract::siRNA based therapeutics is an emerging class of molecules with a high potential for fulfilling the promise of gene medicine. The high selectivity of siRNAs for their targets and subsequent gene ablation has been effectively demonstrated in a wide range of pre-clinical models. siRNA delivery in vivo has been most succ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2011.09.032

    authors: Kapoor M,Burgess DJ,Patil SD

    更新日期:2012-05-01 00:00:00