Bioadhesive polymer/lipid hybrid nanoparticles as oral delivery system of raloxifene with enhancive intestinal retention and bioavailability.


:Raloxifene (RLX) is a second-generation selective estrogen receptor modulator used to treat osteoporosis in postmenopausal women. RLX fails to be developed into injectable dosage forms due to poor solubility. Although oral formulations are clinically available, the lower bioavailability (<2%) embarrasses the pharmaceutists. This work reported a bioadhesive nanosystem intended for oral delivery of RLX to enhance its oral bioavailability and address the formulation challenge. The bioadhesive nanosystem refers to polymer-lipid hybrid nanoparticles made up of Carbopol 940, glyceryl distearate, and TGPS. RLX was solidly encapsulated into bioadhesive nanoparticles (bNPs) through a nanoprecipitation technique along with synchronous desalting of RLX·HCl. The resultant RLX-loaded bNPs (RLX-bNPs) were characterized by particle size, ζ potential, morphology, and entrapment efficiency. The in vitro release and in vivo oral bioavailability of RLX-bNPs in rats were comparatively investigated with RLX-loaded common lipid nanoparticles (RLX-cNPs). The preferred formulation possesses a particle size of 150 nm around with a polydispersity index (PDI) of 0.282. RLX-bNPs exhibited slower drug release than RLX-cNPs owing to the presence of an adhesive layer. After oral administration, RLX-bNPs resulted in significant enhancement in the bioavailability of RLX, up to 556.9% relative to RLX suspensions, while it was merely 244.7% for RLX-cNPs. Cellular testing and ex vivo transport imaging demonstrated that bNPs were endowed with excellent intestinal epithelial affinity and absorbability. Our study affords an alternative option for designing a suitable oral delivery system specific to amphiphobic drugs like RLX·HCl.


Drug Deliv


Drug delivery


Du X,Gao N,Song X




Has Abstract


2021-12-01 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


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

    更新日期:2014-03-01 00:00:00

  • Combinational dual drug delivery system to enhance the care and treatment of gastric cancer patients.

    abstract::Gastric cancer is a frequently occurring cancer with high mortality each year worldwide. Finding new and effective therapeutic strategy against human gastric cancer is still urgently required. Hence, we have established a new method to achieve treatment-actuated modifications in a tumor microenvironment by utilizing s...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Xiao Y,Gao Y,Li F,Deng Z

    更新日期:2020-12-01 00:00:00

  • Controlled-release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components.

    abstract::The objective of this study was to investigate the effect of lipophilic (Compritol 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. T...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Barakat NS,Elbagory IM,Almurshedi AS

    更新日期:2009-01-01 00:00:00

  • Cleavable PEGylation: a strategy for overcoming the "PEG dilemma" in efficient drug delivery.

    abstract::To prolong the circulation time of drug, PEGylation has been widely used via the enhanced permeability and retention (EPR) effect, thereby providing new hope for better treatment. However, PEGylation also brings the "PEG dilemma", which is difficult for the cellular absorption of drugs and subsequent endosomal escape....

    journal_title:Drug delivery

    pub_type: 杂志文章,评审


    authors: Fang Y,Xue J,Gao S,Lu A,Yang D,Jiang H,He Y,Shi K

    更新日期:2017-12-01 00:00:00

  • Strategies for meloxicam delivery to and across the skin: a review.

    abstract::Although meloxicam (MX) is relatively safer than other NSAIDs, adverse effects relating to the gastro-intestinal tract are still a problem when administrated MX at high doses and on the long-term treatment. Drug delivery via skin provides an attractive alternative to oral administration, but is limited by the first la...

    journal_title:Drug delivery

    pub_type: 杂志文章,评审


    authors: Chen J,Gao Y

    更新日期:2016-10-01 00:00:00

  • Graphene oxide enhances alginate encapsulated cells viability and functionality while not affecting the foreign body response.

    abstract::The combination of protein-coated graphene oxide (GO) and microencapsulation technology has moved a step forward in the challenge of improving long-term alginate encapsulated cell survival and sustainable therapeutic protein release, bringing closer its translation from bench to the clinic. Although this new approach ...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Ciriza J,Saenz Del Burgo L,Gurruchaga H,Borras FE,Franquesa M,Orive G,Hernández RM,Pedraz JL

    更新日期:2018-11-01 00:00:00

  • Efficient exosome delivery in refractory tissues assisted by ultrasound-targeted microbubble destruction.

    abstract::Recently, exosomes have been emerged as promising drug delivery carriers, while certain tissues are intrinsically resistant to exosomes. Therapeutically improving the drug delivery efficiency in these tissues/organs would certainly broaden the potential application of exosomes in future. Ultrasound-targeted microbubbl...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Sun W,Li Z,Zhou X,Yang G,Yuan L

    更新日期:2019-12-01 00:00:00

  • Transdermal delivery of vancomycin hydrochloride using combination of nano-ethosomes and iontophoresis: in vitro and in vivo study.

    abstract::This study aimed to evaluate transdermal delivery of vancomycin hydrochloride using the combination of ethosomes as an encapsulating vesicle and iontophoresis. Ethosomes were prepared and evaluated in terms of electrochemical stability. Cathodal iontophoresis of negatively charged ethosomes and anodal iontophoresis of...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Mohammed MI,Makky AM,Teaima MH,Abdellatif MM,Hamzawy MA,Khalil MA

    更新日期:2016-06-01 00:00:00

  • Influence of potential inhalation carriers on stability of thymopentin in rat bronchoalveolar lavage fluid.

    abstract::In the present study, the stability of thymopentin (TP5) in bronchoalveolar lavage fluid (BALF) in presence of potential excipients in inhalation formulation was investigated. The content of TP5 was determined using HPLC method. Commonly used bulking agent, dispersibility enhancers and absorption enhancers in inhalati...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Cai C,Wang L,Dong W,Tang X

    更新日期:2014-09-01 00:00:00

  • Extruded Soluplus/SIM as an oral delivery system: characterization, interactions, in vitro and in vivo evaluations.

    abstract::The aim of this study was to obtain a stable, amorphous solid dispersion (SD) with Soluplus, prepared by hot-melt extrusion (HME) as an effective and stable oral delivery system to improve the physical stability and bioavailability of the poorly water-soluble simvastatin (SIM), a drug with relatively low Tg. The drug ...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Zhang Y,Liu Y,Luo Y,Yao Q,Zhong Y,Tian B,Tang X

    更新日期:2016-07-01 00:00:00

  • Brain-derived neurotrophic factor delivered to the brain using poly (lactide-co-glycolide) nanoparticles improves neurological and cognitive outcome in mice with traumatic brain injury.

    abstract::Currently, traumatic brain injury (TBI) is the leading cause of death or disabilities in young individuals worldwide. The multi-complexity of its pathogenesis as well as impermeability of the blood-brain barrier (BBB) makes the drug choice and delivery very challenging. The brain-derived neurotrophic factor (BDNF) reg...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Khalin I,Alyautdin R,Wong TW,Gnanou J,Kocherga G,Kreuter J

    更新日期:2016-11-01 00:00:00

  • The optimized drug delivery systems of treating cancer bone metastatic osteolysis with nanomaterials.

    abstract::Some cancers such as human breast cancer, prostate cancer, and lung cancer easily metastasize to bone, leading to osteolysis and bone destruction accompanied by a complicated microenvironment. Systemic administration of bisphosphonates (BP) or denosumab is the routine therapy for osteolysis but with non-negligible sid...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Cheng X,Wei J,Ge Q,Xing D,Zhou X,Qian Y,Jiang G

    更新日期:2021-12-01 00:00:00

  • Release of albumin from oligoester plastic matrices: effect of magnesium oxide and bivalent stearates.

    abstract::Biodegradable implantable matrices containing bovine serum albumin were prepared from oligoesters by melting, and subsequently tested on in vitro albumin release. The linear poly (DL-lactic acid) and the branched terpolymer of DL-lactic acid, glycolic acid, and mannitol were synthesized. Products were of similar molec...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Kladnícková I,Dittrich M,Klein T,Pokorová D

    更新日期:2006-01-01 00:00:00

  • Enhanced hepatoprotective activity of andrographolide complexed with a biomaterial.

    abstract:CONTEXT:Humic acid (HA), a natural organic matter is recently being investigated for pharmaceutical purposes. Andrographolide (AGP), a potent hepatoprotective, possesses low aqueous solubility which results in a low bioavailability after oral administration, inappropriate tissue localization and consequently poor thera...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Thingale AD,Shaikh KS,Channekar PR,Galgatte UC,Chaudhari PD,Bothiraja C

    更新日期:2015-01-01 00:00:00

  • Transdermal delivery of isoniazid and rifampin in guinea pigs by electro-phonophoresis.

    abstract::Electro-phonophoresis (EP) has been used as a drug delivery approach in clinical fields. The objective of the present study is to evaluate the skin permeability of isoniazid and rifampin in guinea pigs by EP to provide reference basis for clinical applications of such transdermal delivery system in the treatment of pa...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Chen S,Han Y,Yu D,Huo F,Wang F,Li Y,Dong L,Liu Z,Huang H

    更新日期:2017-11-01 00:00:00

  • Identification and imaging of miR-155 in the early screening of lung cancer by targeted delivery of octreotide-conjugated chitosan-molecular beacon nanoparticles.

    abstract::Lung cancer is still the most common cancer globally. Early screening remains the key to improve the prognosis of patients. There is currently a lack of specific and sensitive methods for early screening of lung cancer. In recent years, studies have found that microRNA plays an important role in the occurrence and dev...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Zhu HZ,Hou J,Guo Y,Liu X,Jiang FL,Chen GP,Pang XF,Sun JG,Chen ZT

    更新日期:2018-11-01 00:00:00

  • Development and characterization of mucoadhesive microspheres bearing salbutamol for nasal delivery.

    abstract::Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In our present work, mucoadhesive chitosan microspheres were prepared by emulsion solvent method. Formulations were characterized for various physicochemical attributes, shape, surface...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Jain SK,Chourasia MK,Jain AK,Jain RK,Shrivastava AK

    更新日期:2004-03-01 00:00:00

  • Transdermal administration of melatonin coupled to cryopass laser treatment as noninvasive therapy for prostate cancer.

    abstract::Melatonin, a pineal gland hormone, exerts oncostatic activity in several types of human cancer, including prostate, the most common neoplasia and the third most frequent cause of male cancer death in the developed world. The growth of androgen-sensitive LNCaP prostate cancer cells in mice is inhibited by 3 mg/kg/week ...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Terraneo L,Bianciardi P,Virgili E,Finati E,Samaja M,Paroni R

    更新日期:2017-11-01 00:00:00

  • A novel drug delivery gel of terbinafine hydrochloride with high penetration for external use.

    abstract:CONTEXT:Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Transfersomes, also known as flexible liposome, could improve transmission of drug for local external use. Terbinafine hydrochloride-loaded liposome is expected to beco...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Yang Y,Ou R,Guan S,Ye X,Hu B,Zhang Y,Lu S,Zhou Y,Yuan Z,Zhang J,Li QG

    更新日期:2015-12-01 00:00:00

  • Orally delivered polycurcumin responsive to bacterial reduction for targeted therapy of inflammatory bowel disease.

    abstract::Inflammatory bowel disease (IBD) such as Crohn's disease and ulcerative colitis is a chronic autoimmune disease affecting nearly five million people worldwide. Among all drug delivery system, oral administration is the most preferable route for colon-specific targeting and the treatment of IBD. Herein, an amphiphilic ...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Qiao H,Fang D,Chen J,Sun Y,Kang C,Di L,Li J,Chen Z,Chen J,Gao Y

    更新日期:2017-11-01 00:00:00

  • Preparation of sodium cholate-based micelles through non-covalent ıbonding interaction and application as oral delivery systems for paclitaxel.

    abstract::In present study, two types of micelles based on sodium cholate (NaC) were prepared through non-covalent bonding interaction and the potential of micelles as oral drug delivery systems for paclitaxel (PTX) was evaluated. Pluronic-chitosan (F127-CS) and Pluronic-poly (acrylic acid) (F127-PAA) copolymers were synthesize...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Ge Y,Zhao Y,Li L

    更新日期:2016-09-01 00:00:00

  • Chemotherapeutic efficacy of nanoparticle encapsulated antitubercular drugs.

    abstract::Our objective was to evaluate the chemotherapeutic potential of oral poly lactide-co-glycolide (PLG, a synthetic polymer) nanoparticle encapsulated ethambutol in combination with PLG-nanoparticle encapsulated-(rifampicin + isoniazid + pyrazinamide) in a murine tuberculosis (TB) model. Our formulation was prepared by t...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Pandey R,Sharma S,Khuller GK

    更新日期:2006-07-01 00:00:00

  • Chitosan-based particles as controlled drug delivery systems.

    abstract::Chitosan, a natural-based polymer obtained by alkaline deacetylation of chitin, is nontoxic, biocompatible, and biodegradable. These properties make chitosan a good candidate for conventional and novel drug delivery systems. This article reviews the approaches aimed to associate bioactive molecules to chitosan in the ...

    journal_title:Drug delivery

    pub_type: 杂志文章,评审


    authors: Prabaharan M,Mano JF

    更新日期:2005-01-01 00:00:00

  • Neuronal mitochondria-targeted therapy for Alzheimer's disease by systemic delivery of resveratrol using dual-modified novel biomimetic nanosystems.

    abstract::Reactive oxygen species (ROS)-induced neuronal mitochondrial dysfunction is a key pathologic factor in sporadic Alzheimer's disease (AD). Neuronal mitochondria have been proposed to be a promising therapeutic target for AD, especially for the failures of phase III clinical trials on conventional amyloid-β (Aβ) targete...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Han Y,Chu X,Cui L,Fu S,Gao C,Li Y,Sun B

    更新日期:2020-12-01 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


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

    更新日期:2011-05-01 00:00:00

  • The challenges of oral drug delivery via nanocarriers.

    abstract::The oral application of pharmaceuticals is unarguably the most convenient method of application. Especially for protein- or peptide-based drugs, however, the effectiveness is significantly reduced due to enzymatic digestion in the stomach as well as a poor bioavailability in the small intestine. For these difficult fo...

    journal_title:Drug delivery

    pub_type: 杂志文章,评审


    authors: Reinholz J,Landfester K,Mailänder V

    更新日期:2018-11-01 00:00:00

  • Poly(HEMA-Zidovudine) conjugate: a macromolecular pro-drug for improvement in the biopharmaceutical properties of the drug.

    abstract::A macromolecular pro-drug of a known anti-viral agent Zidovudine (AZT) was synthesized and evaluated as a sustained drug delivery system. The pro-drug was synthesized by coupling the drug to 2-hydroxyethyl methacrylate (HEMA) through a succinic spacer to get a monomeric drug conjugate which was polymerized to obtain t...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Neeraj A,Chandrasekar MJ,Sara UV,Rohini A

    更新日期:2011-05-01 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


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

    更新日期:2020-12-01 00:00:00

  • Enhanced skin permeation of 6-methoxy-2-naphthylacetic acid by salt formation.

    abstract::The aim of this work was to prepare salts of 6-methoxy-2-naphthylacetic acid (6-MNA) to improve its physicochemical properties for percutaneous application. 6-MNA, an active metabolite of non-steroidal anti-inflammatory drug nabumetone has long half life and has the tendency to penetrate well into synovial fluid. The ...

    journal_title:Drug delivery

    pub_type: 杂志文章


    authors: Pawar V,Kumar HY,Giridhar R,Yadav MR

    更新日期:2015-05-01 00:00:00

  • Formulation and evaluation of dextromethorphan hydrobromide sustained release tablets.

    abstract::Sustained release (SR) matrix tablets of dextromethorphan hydrobromide were prepared by wet granulation using hydroxypropyl methyl cellulose (HPMC-K-100 CR) as the hydrophilic rate controlling polymer. The effect of the concentration of the polymer and different fillers on the in vitro drug release rate was studied. T...

    journal_title:Drug delivery

    pub_type: 杂志文章,随机对照试验


    authors: Meyyanathan SN,Rajan S,Muralidaharan S,Siddaiah MK,Krishnaraj K,Suresh B

    更新日期:2008-09-01 00:00:00