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 inhalation were investigated with respect to the stability of TP5 in BALF. Finally, the stability of TP5 in two inhalation formulations based on the screening experiments was tested in BALF. The results showed that TP5 alone degraded very rapidly in BALF and zero-order enzymatic reaction with a half-life of t0.5 = 49.20 min was observed using 10 times diluted BALF. Among the amino acids examined, leucine and phenylalanine effectively inhibited the enzymolysis of TP5 with prolonged half-life of 112.7 min and 136.2 min, respectively. Nevertheless, slight but insignificant inhibition effect was witnessed for tyrosine, aspartic acid, and lysine; and negligible prevention on the degradation process of TP5 were found for lactose and mannitol. Regarding chitosan, irrespective with molecular weight, the formation of chitosan-TP5 complex improved the stability of TP5 with prolonged t0.5 by 1.8 times. However, along with the improved stability of TP5 in spray-dried chitosan microspheres, the content of TP5 in formulations was reduced to about 75% during preparation process. Thus, leucine was proved to be a prior candidate for inhalation formulation of TP5. Consequently, the results indicate the potential of leucine as carrier for pulmonary delivery of TP5 serving as both stabilizer and dispersibility enhancer.
journal_name
Drug Delivjournal_title
Drug deliveryauthors
Cai C,Wang L,Dong W,Tang Xdoi
10.3109/10717544.2013.878002subject
Has Abstractpub_date
2014-09-01 00:00:00pages
495-500issue
6eissn
1071-7544issn
1521-0464journal_volume
21pub_type
杂志文章相关文献
DRUG DELIVERY文献大全abstract::Administration of influenza vaccines to the lungs could be an attractive alternative to conventional parenteral administration. In this study, we investigated the deposition site of pulmonary delivered liquid and powder influenza vaccine formulations and its relation to their immunogenicity and protective efficacy. In...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2018.1435748
更新日期:2018-11-01 00:00:00
abstract::This study focused on preparation and evaluation of a thermosensitive and mucoadhesive in situ gelling ophthalmic system of azithromycin (ATM). Poloxamer 407 (P407) and poloxamer 188 (P188) were used as gelling agents. Addition of Carbopol 974P (CP 974P) to the gelling systems could increase the solubility of ATM by s...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2010.483255
更新日期:2010-09-01 00:00:00
abstract::Recently, genkwanin (GKA) has been shown to display in vitro antitumor activity against some cancer cells, but its poor solubility restricted the in vivo study and further investigation of its antitumor therapeutic efficacy. In this paper, genkwanin nanosuspensions (GKA-NSps) were successfully prepared using D-alpha t...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2017.1384519
更新日期:2017-11-01 00:00:00
abstract::Endostatin (ES) can effectively inhibit neovascularization in most solid tumors and has the potential to make oxygen delivery more efficient and increase the efficacy of radiotherapy (RT). With a short half-life, ES is mainly administered systemically, which leads to low intake in tumor tissue and often toxic systemic...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2020.1869864
更新日期:2021-12-01 00:00:00
abstract:OBJECTIVE:In the present study, Curcumin (CU)-loaded nanocarrier (NC) such as nanoemulsion (NE) was developed with the objective of increasing its cytotoxicity and bioavailability through lymphatic transport by enhancing its solubility and intestinal permeability. MATERIALS AND METHODS:Based on the area obtained in ps...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2014.909906
更新日期:2016-01-01 00:00:00
abstract::Surface modification of liposomes with polymer to optimize drug delivery was well developed recently. The objective of the present work was to evaluate the feasibility of chitosan-coated liposomes (CSLP) as vehicles for anti-sense oligodeoxynucleotides (ASON). CSLP was obtained by adding chitosan dropwise to liposomes...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2010.549526
更新日期:2011-04-01 00:00:00
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
doi:10.1080/10717544.2020.1745328
更新日期:2020-12-01 00:00:00
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
doi:10.1080/10717544.2018.1501119
更新日期:2018-11-01 00:00:00
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
更新日期:2020-12-01 00:00:00
abstract::Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations. The objective of thi...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2013.843608
更新日期:2014-05-01 00:00:00
abstract::Aminoglycoside-induced hair cell (HC) loss is a major cause of hearing impairment, and the effective prevention of HC loss remains an unmet medical need. Epigenetic mechanisms have been reported to be involved in protecting cochlear cells against ototoxic drug injury, and in this study we developed new bioactive compo...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2018.1461277
更新日期:2018-11-01 00:00:00
abstract::A new strategy based on gastric retention is proposed for the treatment of Helicobacter pylori. (H. pylori). A synergism between a floating and a bioadhesive system has been explored. Floating microspheres containing the antiurease drug acetohydroxamic acid (AHA) were prepared by a novel quasi-emulsion solvent diffusi...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717540260397837
更新日期:2002-10-01 00:00:00
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
doi:10.3109/10717544.2014.960982
更新日期:2016-07-01 00:00:00
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
更新日期:2020-12-01 00:00:00
abstract::Glycyrrhizin or glycyrrhizic acid (GA) - triterpene glycoside extracted from licorice root - has been intensively studied over the past decade and is considered to be a potential drug delivery system. Glycyrrhizin was found to enhance the therapeutic effect of various drugs; however the detailed mechanism of these eff...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2014.919544
更新日期:2016-01-01 00:00:00
abstract::Bone metastasis is a devastating complication of cancer that requires an immediate attention. Although our understanding of the metastatic process has improved over the years, yet a number of questions still remain unanswered, and more research is required for complete understanding of the skeletal consequences of met...
journal_title:Drug delivery
pub_type: 杂志文章,评审
doi:10.3109/10717544.2014.913325
更新日期:2016-01-01 00:00:00
abstract::Ketorolac tromethamine, a potent nonnarcotic analgesic agent and 800 times more potent than aspirin, is indicated for the short-term management of moderate to such severe painful states as post operative pain, acute musculoskeletal pain, and dental pain. It Given every 6 hr intramuscularly in patients for acute pain, ...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717540500398092
更新日期:2008-08-01 00:00:00
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
doi:10.3109/10717544.2015.1013200
更新日期:2016-06-01 00:00:00
abstract::This work evaluates solid lipid nanoparticles of thiopental sodium against obesity-induced cardiac dysfunction and hypertrophy and explores the possible mechanism of action. TS loaded SLNs were formulated by hot-homogenization and solvent diffusion method. TS-SLNs were scrutinized for entrapment efficiency, drug loadi...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2020.1803449
更新日期:2020-12-01 00:00:00
abstract::The distinct hormone molecules and receptors, such as follicle-stimulating hormone receptor (FSHR) in ovarian cancer, provide opportunities for more precisely targeted therapy. We previously developed FSHR-mediated nanoparticles and found that FSH peptides on the surface of nanoparticles improved the delivery of short...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2018.1440667
更新日期:2018-11-01 00:00:00
abstract::S-nitrosothiols are a class of NO-donors currently under investigation for the treatment of various diseases. In this study, we developed a novel NO-donor (S-nitrosoglutathione-alginate, SNA) by cross-linking alginate with S-nitrosothiols, which can deliver NO in a sustained manner. This compound can be further evalua...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2015.1122676
更新日期:2016-10-01 00:00:00
abstract::The aim of this work was to encapsulate superoxide dismutase (SOD) into biodegradable microparticles by spray-drying technique. The nature of the organic solvent to dissolve the polymer, the method of incorporation of the drug in the organic phase (with or without a surfactant, namely sucrose ester of HLB = 6), the su...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717540490280363
更新日期:2004-05-01 00:00:00
abstract::The effects of various vehicles and adhesives on the percutaneous absorption of isosorbide dinitrate (ISDN) were evaluated. Lauroglycol FCC showed the highest flux among vehicles tested. The flux of ISDN from silicone and acrylic adhesive matrices was found to be higher than that from other types of adhesive matrices....
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10426500290095430
更新日期:2002-04-01 00:00:00
abstract:CONTEXT:Intraoral drug delivery as mucosal delivery pathway provides a huge platform in the pharmaceutical field. OBJECTIVE:Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery. MATERIALS AND METHODS:Mediated by carbodiimide, cysteine was covalentl...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.3109/10717544.2015.1122673
更新日期:2016-07-01 00:00:00
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
doi:10.1080/10717540802035301
更新日期:2008-09-01 00:00:00
abstract::To improve drug retention in carriers for amphiphilic asulacrine (ASL), a novel active loading method using micelle gradient was developed to fabricate the ASL-loaded multiseed liposomes (ASL-ML). The empty ML were prepared by hydrating a thin film with empty micelles. Then the micelles in liposomal compartment acting...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2018.1440669
更新日期:2018-11-01 00:00:00
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
更新日期:2020-12-01 00:00:00
abstract::Small interfering RNA (siRNA) exhibits great potential as a novel therapeutic option due to its highly sequence-specific ability to silence genes. However, efficient and safe delivery carriers are required for developing novel therapeutic paradigms. Thus, the successful development of efficient delivery platforms for ...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2019.1667452
更新日期:2020-12-01 00:00:00
abstract::The ophthalmic drug delivery is a challenge in the clinical treatment of ocular diseases. The traditional drug administration usually shows apparent limitations, such as the low bioavailability from the reason of low penetration of the cornea and the short survival time of drug in the eyes. To overcome these shortcomi...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717544.2018.1474972
更新日期:2018-11-01 00:00:00
abstract::Nonviral gene delivery systems are a promising approach for gene therapy applications, despite their low in vivo gene transfer efficiency. One approach to enhance this efficiency is to incorporate targeting elements into cationic lipid/DNA complexes (lipoplexes). Ligand-containing lipoplexes have to retain their effic...
journal_title:Drug delivery
pub_type: 杂志文章
doi:10.1080/10717540490265405
更新日期:2004-11-01 00:00:00