Inhalable Microparticles as Carriers for Pulmonary Delivery of Thymopentin-Loaded Solid Lipid Nanoparticles.
Summary of "Inhalable Microparticles as Carriers for Pulmonary Delivery of Thymopentin-Loaded Solid Lipid Nanoparticles."
PURPOSE:
Microparticles containing solid lipid nanoparticles (SLNs) are receiving increased attention as carriers for the lung delivery of the SLNs. Thus, we aim to prepare the hybrid microparticles and thoroughly evaluate their feasibility for the pulmonary drug delivery.
METHODS:
The microparticles were prepared by co-spray-drying the thymopentin (TP5)-loaded SLNs with bulking agents. Thereafter, we systematically estimated the potential of the microparticles as the carriers for the pulmonary delivery of the SLNs, including the investigations of their characteristics, aerodynamic properties, pharmacokinetics and pharmacodynamics.
RESULTS:
The spherical and hollow microparticles presented a size of 4.1 +/- 0.1 mum and a low tap density of 0.175 +/- 0.02 g/cm(3). In addition, the microparticles showed a high aerosolization efficiency (emitted dose of 98.0% +/- 1.23% and respirable fraction of 51.07% +/- 1.21%). Furthermore, the SLNs could be easily recovered from the microparticles without essential changes on their characteristics and the drug release behavior. The pharmacokinetic and pharmacodynamic studies suggested that, compared to i.v. TP5 solution, the bioavailability and therapeutic efficacy of TP5 were remarkably strengthened after the pulmonary administration of the microparticles.
CONCLUSIONS:
Taken together, we believe the microparticles were suitable for inhalation and possesed an ample potential for the pulmonary delivery of the SLNs.
Affiliation
Key Laboratory of Drug Targeting and Novel Drug Delivery Systems West China School of Pharmacy, Sichuan University, No. 17, Block 3, Southern Renmin Road, Chengdu, 610041, People's Republic of China.
Journal Details
This article was published in the following journal.
Name: Pharmaceutical research
ISSN: 1573-904X
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20625801
- DOI: http://dx.doi.org/10.1007/s11095-010-0201-z
Medical and Biotech [MESH] Definitions
Drug Carriers
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
Cell-derived Microparticles
Extracellular membrane vesicles generated by the shedding of CELL MEMBRANES blebs. Microparticles originating from PLATELETS; ENDOTHELIAL CELLS; and other cell types circulate in the peripheral blood and through the MICROVASCULATURE where larger cells cannot, functioning as active effectors in a variety of vascular processes such as INFLAMMATION; HEMOSTASIS; angiogenesis; and vascular reactivity. Increased levels are found following stimulation of bleb formation under normal or pathological conditions.
Pulmonary Sclerosing Hemangioma
A benign neoplasm of pneumocytes, cells of the PULMONARY ALVEOLI. Originally considered to be vascular in origin, it is now classified as an epithelial tumor with several elements, including solid cellular areas, papillary structure, sclerotic regions, and dilated blood-filled spaces resembling HEMANGIOMA.
Pulmonary Heart Disease
Hypertrophy and dilation of the RIGHT VENTRICLE of the heart that is caused by PULMONARY HYPERTENSION. This condition is often associated with pulmonary parenchymal or vascular diseases, such as CHRONIC OBSTRUCTIVE PULMONARY DISEASE and PULMONARY EMBOLISM.
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.
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