Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems: in vitro, in vivo and in situ intestinal permeability studies.

Abstract:

:The main purpose of this work was to develop and evaluate a self-emulsifying drug delivery system (SEDDS) of piperine to enhance its solubility and bioavailability. The formulation was optimized by solubility test and ternary phase diagrams. Then physiochemical properties and in vitro release of SEDDS were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of SEDDS on the bioavailability and intestinal absorption of piperine. The optimized formulation was composed of ethyl oleate, Tween 80 and Transcutol P (3:5.5:1.5, w/w), with the level of the piperine reached 2.5% (w/w). The in vitro dissolution rates of piperine SEDDS were significantly higher than the self-prepared capsules. In vivo pharmacokinetic study showed Cmax1, Cmax2 and area under the curve of piperine after oral administration of SEDDS in rats were 3.8-, 7.2- and 5.2-fold higher than the self-prepared capsules, respectively, and the relative bioavailability of SEDDS was 625.74%. The in situ intestinal absorption study revealed that the effective permeability and the effective absorption rate values of piperine for SEDDS were significantly improved comparing to solutions (p < 0.01). So SEDDS formulation could improve the oral bioavailability and intestinal absorption of piperine effectively.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Shao B,Cui C,Ji H,Tang J,Wang Z,Liu H,Qin M,Li X,Wu L

doi

10.3109/10717544.2014.898109

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

740-7

issue

6

eissn

1071-7544

issn

1521-0464

journal_volume

22

pub_type

杂志文章
  • Preparation and characterization of solid lipid nanoparticles containing cloricromene.

    abstract::This article describes the development of solid lipid nanoparticles (SLN) as colloidal carriers for cloricromene. Nanoparticles were prepared by the microemulsion or precipitation technique. In vitro drug release profile from SLN was studied under various experimental conditions mimicking some body fluids. The drug re...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/drd_10_4_245

    authors: Bondì ML,Fontana G,Carlisi B,Giammona G

    更新日期:2003-10-01 00:00:00

  • Optimizing novel penetration enhancing hybridized vesicles for augmenting the in-vivo effect of an anti-glaucoma drug.

    abstract::Usually the topical delivery of ocular drugs poses a great challenge. Accordingly, the work in this study comprised the use of different hybrids of generally regarded as safe (GRAS) oils and surfactants in order to develop and optimize novel acetazolamide (AZD) entrapped-vesicular systems aiming at improving its ocula...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2016.1233588

    authors: Naguib SS,Hathout RM,Mansour S

    更新日期:2017-11-01 00:00:00

  • Drug product development and pharmacological evaluation of a sparingly soluble novel camptothecin analog for peroral administration.

    abstract::This work focused on the developmental aspects, pharmacokinetic evaluation, and pharmacological assessment of a drug inclusion complex for a novel camptothecin analog (CA) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). Camptothecins analog belong to topoisomerase-I inhibitor class of compounds with proven anti-tumor ac...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2010.544689

    authors: Nekkanti V,Karatgi P,Paruchuri S,Pillai R

    更新日期:2011-05-01 00:00:00

  • Mometasone furoate-loaded cold processed oil-in-water emulsions: in vitro and in vivo studies.

    abstract::Over the years, research has focused on strategies to increase benefit/risk ratio of corticoids. However, vehicles intended for topical glucocorticoids delivery with an improved benefit/risk ratio are still on demand. The aim of this work was the in vitro and in vivo characterization of cold processed oil-in-water (o/...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.871086

    authors: Raposo S,Tavares R,Gonçalves L,Simões S,Urbano M,Ribeiro HM

    更新日期:2015-01-01 00:00:00

  • Chitosan-N-acetyl cysteine conjugates: in vitro evaluation of permeation enhancing and P-glycoprotein inhibiting properties.

    abstract::This study evaluated three chitosan-N-acetyl cysteine (CAC) conjugates of increasing molecular mass as a valuable tool to improve the absorption of drugs by assessing its permeation enhancing effect regarding the active P-gp substrate rhodamine-123 in comparison to the trans- and paracellular marker FD 4 both in rat i...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540802006708

    authors: Schmitz T,Hombach J,Bernkop-Schnürch A

    更新日期:2008-05-01 00:00:00

  • Effects of bile salts on the lovastatin pharmacokinetics following oral administration to rats.

    abstract::This study aimed to examine the effects of bile salts on pharmacokinetics of lovastatin, which has low bioavailability. Lovastatin solid dispersions were prepared using sodium deoxycholate (NaDC) and sodium glycholate (NaGC) at ratios of 1:19, 1:49, and 1:69. The formulated solid dispersions and control (commercial ta...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2010.512024

    authors: Kim K,Yoon I,Chun I,Lee N,Kim T,Gwak HS

    更新日期:2011-01-01 00:00:00

  • A novel ligand conjugated nanoparticles for oral insulin delivery.

    abstract::In order to enhance the interaction between nanocarrier and gastrointestinal epithelial cells, we developed nanoparticles (NPs) modified with targeting ligand FQSIYPpIK (FQS), which specifically interact with integrin αvβ3 receptor expressing on the intestinal epithelium. The targeting NPs were prepared by coating the...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1058433

    authors: Liu C,Shan W,Liu M,Zhu X,Xu J,Xu Y,Huang Y

    更新日期:2016-07-01 00:00:00

  • Sodium alginate microspheres of metoprolol tartrate for intranasal systemic delivery: development and evaluation.

    abstract::Bioadhesive sodium alginate microspheres of Metoprolol tartrate (MT) for intranasal systemic delivery were prepared to avoid the first-pass effect, as an alternative therapy to injection, and to obtain improved therapeutic efficacy in the treatment of hypertension and angina pectoris. The microspheres (Ms) were prepar...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/713840323

    authors: Rajinikanth PS,Sankar C,Mishra B

    更新日期:2003-01-01 00:00:00

  • Effects of phonophoresis with gold nanoparticles on oxidative stress parameters in a traumatic muscle injury model.

    abstract::The aim of this study was to evaluate the effects of therapeutic pulsed ultrasound with gold nanoparticles on oxidative stress parameters after traumatic muscle injury in Wistar rats. The animals were randomly divided into nine groups (n = 6 each): sham (uninjured muscle); muscle injury without treatment; muscle injur...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2014.923063

    authors: Silveira PC,Victor EG,Notoya Fde S,Scheffer Dda L,Silva Ld,Cantú RB,Martínez VH,de Pinho RA,Paula MM

    更新日期:2016-01-01 00:00:00

  • Formulation of Fe3O4/acrylate co-polymer nanocomposites as potential drug carriers.

    abstract::Magnetic nanocomposite particles were synthesized by encapsulating nanosized magnetite with an acrylate-based cationic co-polymer made of MMA, BA, and QMA and modifying with MeOPEGMA using the water replacement method. The composition of the co-polymer formulation was optimized based on zeta-potential measurements and...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540801952597

    authors: Phanapavudhikul P,Shen S,Ng WK,Tan RB

    更新日期:2008-03-01 00:00:00

  • Development and characterization of sponge-like acyclovir ocular minitablets.

    abstract::For the treatment of ocular keratitis acyclovir, as a highly specific inhibitor of herpes virus replication, is applied topically into the eye. The objective of this study was to design and evaluate freeze-dried, bioadhesive and biodegredable acyclovir ocular minitablets for prolonged local drug action. The sponge-lik...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2010.509364

    authors: Refai H,Tag R

    更新日期:2011-01-01 00:00:00

  • In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids.

    abstract::Improvement of water solubility, dissolution rate, oral bioavailability, and reduction of first pass metabolism of OL (OL), were the aims of this research. Co-amorphization of OL carboxylic acid dispersions at various molar ratios was carried out using rapid solvent evaporation. Characterization of the dispersions was...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2016.1153746

    authors: Maher EM,Ali AM,Salem HF,Abdelrahman AA

    更新日期:2016-10-01 00:00:00

  • Preparation of N,O-carboxymethyl chitosan nanoparticles as an insulin carrier.

    abstract::The aim of this research was to develop pH-sensitive insulin-loaded NOCC (N,O-carboxymethyl chitosan) nanoparticles for the controlled release of insulin via the oral route. Thus, in this study, insulin-loaded NOCC nanoparticles were prepared by ionic gelation of NOCC with TPP (tripolyphosphate). NOCC nanoparticles we...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717540903353090

    authors: Lin CC,Lin CW

    更新日期:2009-11-01 00:00:00

  • Liraglutide-loaded multivesicular liposome as a sustained-delivery reduces blood glucose in SD rats with diabetes.

    abstract::Subcutaneous liraglutide-loaded multivesicular liposomes (Lrg-MVLs) were developed as a sustained drug-delivery system for treating diabetes and their properties were characterized. The Lrg-MVLs prepared using a two-step water-in-oil-in-water double emulsification process had a spherical appearance with a mean diamete...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2016.1180723

    authors: Zhang L,Ding L,Tang C,Li Y,Yang L

    更新日期:2016-11-01 00:00:00

  • Brain targeted oral delivery of doxycycline hydrochloride encapsulated Tween 80 coated chitosan nanoparticles against ketamine induced psychosis: behavioral, biochemical, neurochemical and histological alterations in mice.

    abstract::To develop statistically optimized brain targeted Tween 80 coated chitosan nanoparticulate formulation for oral delivery of doxycycline hydrochloride for the treatment of psychosis and to evaluate its protective effect on ketamine induced behavioral, biochemical, neurochemical and histological alterations in mice. 32 ...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2017.1377315

    authors: Yadav M,Parle M,Sharma N,Dhingra S,Raina N,Jindal DK

    更新日期:2017-11-01 00:00:00

  • In vitro assessment of lidocaine release from aqueous and oil solutions and from preformed and in situ formed aqueous and oil suspensions. Parenteral depots for intra-articular administration.

    abstract::In vitro drug release rates from aqueous and oil solutions as well as preformed and in situ formed aqueous and oil suspensions intended for intra-articular delivery have been investigated using the rotating dialysis cell model. Using lidocaine as a model drug substance the release kinetics from aqueous and oil suspens...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540701828657

    authors: Pedersen BT,Larsen SW,Østergaard J,Larsen C

    更新日期:2008-01-01 00:00:00

  • Formulation and in vivo assessment of terconazole-loaded polymeric mixed micelles enriched with Cremophor EL as dual functioning mediator for augmenting physical stability and skin delivery.

    abstract::The aim of the current study was to formulate terconazole (TCZ) loaded polymeric mixed micelles (PMMs) incorporating Cremophor EL as a stabilizer and a penetration enhancer. A 23 full factorial design was performed using Design-Expert® software for the optimization of the PMMs which were formulated using Pluronic P123...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2018.1436098

    authors: Abd-Elsalam WH,El-Zahaby SA,Al-Mahallawi AM

    更新日期:2018-11-01 00:00:00

  • Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl-β-cyclodextrin.

    abstract::Enrofloxacin, a third-generation fluoroquinolone, is a broad-spectrum antimicrobial drug against a lot of veterinary bacterial diseases. However, bactericidal activity of enrofloxacin is concentration-dependent and its poor aqueous solubility and bitter taste limit its development and application. Meanwhile, 2-hydroxy...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1724210

    authors: Ding Y,Pang Y,Vara Prasad CVNS,Wang B

    更新日期:2020-12-01 00:00:00

  • Effect of microemulsion in topical sertaconazole hydrogel: in vitro and in vivo study.

    abstract:PURPOSE:A topical microemulsion (ME)-based hydrogel was developed to enhance permeation of an antifungal drug, sertaconazole (STZL) for effective eradication of cutaneous fungal infection. METHODS:Pseudo-ternary phase diagrams were used to determine the existence of MEs region. ME formulations were prepared with oleic...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2014.914601

    authors: Sahoo S,Pani NR,Sahoo SK

    更新日期:2016-01-01 00:00:00

  • Combined treatment with ultrasound-targeted microbubble destruction technique and NM-aFGF-loaded PEG-nanoliposomes protects against diabetic cardiomyopathy-induced oxidative stress by activating the AKT/GSK-3β1/Nrf-2 pathway.

    abstract::The present study sought to investigate the effect of non-mitogenic acidic fibroblast growth factor (NM-aFGF) loaded PEGylated nanoliposomes (NM-aFGF-PEG-lips) combined with the ultrasound-targeted microbubble destruction (UTMD) technique on modulating diabetic cardiomyopathy (DCM)and the mechanism involved. Animal st...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1785052

    authors: Zhang M,Zhu NW,Ma WC,Chen MJ,Zheng L

    更新日期:2020-12-01 00:00:00

  • Assessment of the efficacy of drug transdermal delivery by electro-phonophoresis in treating tuberculous lymphadenitis.

    abstract::Electro-phonophoresis (EP) has been used in various clinical fields. The objective of present study is to evaluate the skin permeability of isoniazid (INH) and rifampicin (RIF) in patients with tuberculous lymphadenitis with the aid of EP to validate the clinical applications of this transdermal delivery system for th...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1124474

    authors: Chen S,Qin M,Han Y,Zhao L,Fu Y,Shang Y,Liu Z,Huang H

    更新日期:2016-06-01 00:00:00

  • In vitro evaluation of enrofloxacin-loaded MLV liposomes.

    abstract::Fluoroquinolones are broad-spectrum antimicrobial agents that seem to reach their intracellular target site (DNA gyrase) in Escherichia coli by means of an uptake process through the outer and inner membranes. Delivery of quinolones with liposomes has many advantages than the free form of the drug. Liposomes may repre...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540600640146

    authors: Sezer AD,Akbuğa J,Baş AL

    更新日期:2007-01-01 00:00:00

  • A photo-responsive peptide- and asparagine-glycine-arginine (NGR) peptide-mediated liposomal delivery system.

    abstract::The conjugation of tunable peptides or materials with nanocarriers represents a promising approach for drug delivery to tumor cells. In this study, we report the development of a novel liposomal carrier system that exploits the cell surface binding synergism between photo-sensitive peptides (PSPs) and targeting ligand...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1008707

    authors: Xie X,Yang Y,Yang Y,Zhang H,Li Y,Mei X

    更新日期:2016-09-01 00:00:00

  • Floating microspheres of carvedilol as gastro retentive drug delivery system: 3(2) full factorial design and in vitro evaluation.

    abstract:CONTEXT:Designing a sustained release system for Carvedilol to increase its residence time in the stomach. OBJECTIVE:Preparation of floating microsphere by the emulsion solvent diffusion method, studying the effect of various process parameters and optimize the formulation using full factorial design. METHODS:Differe...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.834414

    authors: Nila MV,Sudhir MR,Cinu TA,Aleykutty NA,Jose S

    更新日期:2014-03-01 00:00:00

  • Combined photodynamic-chemotherapy investigation of cancer cells using carbon quantum dot-based drug carrier system.

    abstract::The combined chemotherapy and photodynamic therapy have significant advantages for cancer treatments, which have higher therapeutic effects compared with other medicines. Herein, we focused on the synthesis of carbon quantum dot (CQD) based nanocarrier system. CQD and 5-aminolevulinic acid (5-ALA) were conjugated with...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1765431

    authors: Li X,Vinothini K,Ramesh T,Rajan M,Ramu A

    更新日期:2020-12-01 00:00:00

  • Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats.

    abstract:OBJECTIVE:Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral d...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1039666

    authors: Ansari MJ,Anwer MK,Jamil S,Al-Shdefat R,Ali BE,Ahmad MM,Ansari MN

    更新日期:2016-07-01 00:00:00

  • Preparation and characterization of novel anti-inflammatory biological agents based on piroxicam-loaded poly-ε-caprolactone nano-particles for sustained NSAID delivery.

    abstract::Piroxicam (PX), a main member of non-steroidal anti-inflammatory drugs (NSAIDs), is mainly used orally, which causes side effects of the gastrointestinal tract. It also has systemic effects when administered intramuscularly. Intra-articular (IA) delivery and encapsulation of PX in biodegradable poly-ε-caprolactone (PC...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1716881

    authors: Rahmani Del Bakhshayesh A,Akbarzadeh A,Alihemmati A,Tayefi Nasrabadi H,Montaseri A,Davaran S,Abedelahi A

    更新日期:2020-12-01 00:00:00

  • Synergism of cisplatin-oleanolic acid co-loaded hybrid nanoparticles on gastric carcinoma cells for enhanced apoptosis and reversed multidrug resistance.

    abstract::Combined administration of different drugs is a widely acknowledged approach for effective cancer therapy. However, the limited targeting, as well as inferior drug loading capacities of current drug delivery systems (DDS), are still the bottleneck for better performance in cancer treatment. Herein, we successfully dev...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2019.1710622

    authors: Li D,Cui R,Xu S,Liu Y

    更新日期:2020-12-01 00:00:00

  • Development and characterization of glimepiride nanocrystal formulation and evaluation of its pharmacokinetic in rats.

    abstract::In this paper, orally nanocrystal capsules were produced using nanocrystal formulations in order to optimize dissolution properties of poorly soluble drug glimepiride and improve its bioavailability. The important preparation variables, such as stabilizers, the power input and the time length of ultrasonication on the...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2012.742939

    authors: Du B,Shen G,Wang D,Pang L,Chen Z,Liu Z

    更新日期:2013-01-01 00:00:00

  • Chitosan-based liposomal thermogels for the controlled delivery of pingyangmycin: design, optimization and in vitro and in vivo studies.

    abstract::Pingyangmycin (PYM) has been applied clinically for many years to treat vascular malformations (VM) in China. The major limitation of PYM injections is quick diffusion from the injection site, which increases side effects, especially the possibility of pulmonary injury. In this paper, chitosan/glycerophosphate disodiu...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2018.1444684

    authors: Zhang L,Chen F,Zheng J,Wang H,Qin X,Pan W

    更新日期:2018-11-01 00:00:00