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1.
J Pharm Sci ; 107(9): 2451-2456, 2018 09.
Article in English | MEDLINE | ID: mdl-29883664

ABSTRACT

Salvianolic acids and tanshinones both exhibit efficacy in treating idiopathic pulmonary fibrosis (IPF), but their formulation limits their clinical use. This study aimed to prepare the salvianolic acids and tanshinones dry powder for inhalation (SPI) to achieve pulmonary delivery for the treatment of IPF. The variable quantities of salvianolic acids and tanshinones composite powder were optimized using the central composite design-response surface method. Different carriers with various drug-carrier ratios were optimized to prepare SPI. The final optimized formulation of SPI was as follows: InhaLac 230® was selected as the carrier with drug:carrier = 1:6, and the milled lactose InhaLac 400® was added at 5%. The developed SPI characterized with an angle of repose 52.46 ± 1.04°, Carr's index of 34.00 ± 0.50% and showed high lung deposition in vitro, indicating the potential of pulmonary delivery for the treatment of IPF.


Subject(s)
Abietanes/chemical synthesis , Abietanes/standards , Alkenes/chemical synthesis , Alkenes/standards , Dry Powder Inhalers/standards , Polyphenols/chemical synthesis , Polyphenols/standards , Quality Control , Chemistry, Pharmaceutical/methods
2.
Clin Mater ; 16(4): 177-87, 1994.
Article in English | MEDLINE | ID: mdl-10184316

ABSTRACT

Samples based on ethylene-propylene rubber (EPR) have been surface grafted with acrylamide (AAm) and 2-hydroxyethyl methacrylate (HEMA) using CO2-pulsed laser as a stimulation source. Scanning electron microscopy (SEM), energy dispersive X-ray analysis (EDXA) and attenuated total reflectance infrared (ATR-IR) spectra were performed on the modified samples. These techniques revealed the formation of grafted poly(AAm) and poly(HEMA) on the surface of EPR. The surface grafted poly(AAm) and poly(HEMA) were found to have a fractal type of morphology. EDXA showed insignificant grafted AAm and HEMA in regions where fractals were absent. Fractal patterned surfaces provide hydrophilic and hydrophobic sites, making EPR suitable as a biomaterial. In-vitro adhesion and spreading of alveolar macrophages (AMs) cultured on the surface of modified samples have been evaluated by hemocytometry and SEM, respectively, and compared with unmodified controls. Relationships between AM adhesion and their spreading, with surface morphology, graft level and water compatibility are also discussed. Generally, more AMs attach onto unmodified surfaces with a greater degree of spreading, than on the modified EPR. Samples grafted between 0.7 mg/cm2 and 1 mg/cm2 showed fairly low AM density compared with both unmodified EPR and lightly modified samples (less than 0.2 mg/cm2). AMs cultured on the unmodified EPR were larger and displayed pronounced ruffling of the plasma membrane, an increased capacity for adherence and spreading on the surface, and an increased number of extensive filopodia. Moreover, AMs attached onto the surface of modified samples appeared rounded, with minimal cytoplasmic spreading and ruffling.


Subject(s)
Acrylamides/standards , Alkenes/standards , Ethylenes/standards , Lasers , Methacrylates/standards , Rubber/standards , Absorptiometry, Photon , Acrylamide , Animals , Cell Adhesion/physiology , Fractals , Macrophages, Alveolar/physiology , Materials Testing , Mice , Microscopy, Electron, Scanning , Spectrophotometry, Infrared
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