Nanotechnology versus other techniques in improving drug dissolution

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Delivery of inhalation drugs to children for asthma and other respiratory diseases

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Spray dried oleanolic acid powder for pulmonary delivery

Poster Presentation: no. 13PS51The abstract of the poster presentation is located at http://inhalationasia.org/index.php/poster-presentations/176-13ps51-shuangning-chenIntroduction: Oleanolic acid (OA), well known for its hepatoprotective effect, has been shown in vitro to be cytotoxic in A549 human non-small-cell lung cancer cell line. Thus it may be potentially useful for lung cancer treatment. Being a BCS Class IV drug, it has low oral bioavailability. Therefore, inhalation is the preferred route of administration for local delivery. The aim of this study is to develop an inhalable oleanolic acid dry powder formulation .....published_or_final_versio

Effect of crystallinity on electrostatic charging in DPI formulations

Poster Presentation: no. 13PS41Introduction: Many physicochemical, mechanical and environmental factors can influence charging of dry powder inhaler (DPI) formulations - crystallinity is one of these factors. Due to differences in crystal packing and surface energies, there may be differences in charge transfer behaviours between amorphous and crystalline materials. Although the effect of crystallinity on electrostatic charging in DPI formulations has been investigated previously by other researchers, the reported data were inconclusive since the samples not only differed in crystallinity, but also in particle morphology and size distributions. Therefore, these variables are controlled in the present study to determine the role of crystallinity in electrostatic charging of DPI formulations. The objective of this study was to characterize inherent charges generated by amorphous and crystalline micron-sized salbutamol sulfate (SS) powders .....published_or_final_versio

Delivery of high solubility polyols by vibrating mesh nebuliser to enhance mucociliary clearance

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Oleanolic Acid Delivery using Biodegradable Nanoparticles for Cancer Therapy

Poster PresentationOleanolic acid (OA) is a naturally occurring pentacyclic triterpenoid widely found in Chinese herbs. It has been extensively studied owing to the beneficial effects such as hepatoprotection, anti-inflammatory and it is recently found to have anti-tumor ability. However, resembling the other hydrophobic drugs, it has poor water solubility and therefore very limited intestinal absorption when administrated orally. Investigations concerning the delivery of OA have been carried out to enhance its dissolution and bioavailability. Nanoparticulate systems involve the reduction of drug particle size into nano-scale thereby increasing the interfacial surface area. As a result, absorption of drug in the body system could be enhanced. Biodegradable polymer-based system can be metabolized by the body system into harmless compounds so it is regarded safe and promising. This study was conducted to evaluate the efficacy of four types of biodegradable copolymers as potential OA delivery nanoparticulate system. Co-polymers consisting a hydrophilic block: poly(ethylene) glycol (PEG) and a hydrophobic block of either poly(lactic-co-glycolic) acid (PLGA) or poly(lactic acid) (PLA) were used to fabricate a novel nanoformulation to improve OA bioavailability. The OA-loaded mPEG-(D,L)PLA, mPEG-(L)PLA, mPEG-(D,L)PLGA and mPEG- (L)PLGA nanoparticles (NPs), prepared by nanoprecipitation, were observed to be spherical in shape under transmission electron microscope. Results indicated that narrow size distributed NPs with mean hydrodynamic diameter of 200±16.0, 233±13.9, 211±10.1 and 229±10.1nm respectively were obtained. mPEG-(D,L)PLA NPs attained the highest encapsulation of OA with 75.8% efficiency while mPEG-(L)PLGA NPs displayed the lowest encapsulation efficiency at 40.8%. The in vitro anti-tumoral activity was evaluated on A549, lung carcinoma epithelial cell lines using MTT assay. All the four types of OA-loaded NPs demonstrated better anti-cancer ability than saturated OA in medium. Moreover, NPs without OA exhibited significantly lower cytotoxicity towards A549 indicating induced cell death was due to the effective delivery of OA as an anti-cancer therapeutic agent.published_or_final_versio

Design of dry powder formulations of pH responsive peptide/plasmid DNA complexes for pulmonary delivery

Poster Presentation: no. 13PS50Respiratory diseases are substantial public health problems around the world. Recently, nucleic acid was developed as a potential therapeutic strategy to tackle a series of lung diseases. Delivery still poses one of the major challenges for their clinical application. pH responsive peptides containing either histidine or derivatives of 2,3-diaminopropionic acid (Dap) can mediate effective DNA transfection in lung epithelial cells with the latter remaining effective even in the presence of lung surfactant containing bronchoalveolar fluid (BALF), which make them promising vectors for delivering therapeutic nucleic acid to the airways .....published_or_final_versio

Spray freeze drying of small nucleic acids as inhaled powder for pulmonary delivery

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Bioactive proteins and peptides isolated from Chinese medicines with pharmaceutical potential.

Some protein pharmaceuticals from Chinese medicine have been developed to treat cardiovascular diseases, genetic diseases, and cancer. Bioactive proteins with various pharmacological properties have been successfully isolated from animals such as Hirudo medicinalis (medicinal leech), Eisenia fetida (earthworm), and Mesobuthus martensii (Chinese scorpion), and from herbal medicines derived from species such as Cordyceps militaris, Ganoderma, Momordica cochinchinensis, Viscum album, Poria cocos, Senna obtusifolia, Panax notoginseng, Smilax glabra, Ginkgo biloba, Dioscorea batatas, and Trichosanthes kirilowii. This article reviews the isolation methods, molecular characteristics, bioactivities, pharmacological properties, and potential uses of bioactive proteins originating from these Chinese medicines.published_or_final_versio

Pharmacokinetic and pharmacodynamic study of intranasal and intravenous dexmedetomidine

Background: Intranasal dexmedetomidine produces safe, effective sedation in children and adults. It may be administered by drops from a syringe or by nasal mucosal atomization (MAD NasalTM). / Methods: This prospective, three-period, crossover, double-blind study compared the pharmacokinetic (PK) and pharmacodynamic (PD) profile of i.v. administration with these two different modes of administration. In each session each subject received 1 μg kg−1 dexmedetomidine, either i.v., intranasal with the atomizer or intranasal by drops. Dexmedetomidine plasma concentration and Ramsay sedation score were used for PK/PD modelling by NONMEM. / Results: The i.v. route had a significantly faster onset (15 min, 95% CI 15–20 min) compared to intranasal routes by atomizer (47.5 min, 95% CI 25–135 min), and by drops (60 min, 95%CI 30–75 min), (P<0.001). There was no significant difference in sedation duration across the three treatment groups (P=0.88) nor in the median onset time between the two modes of intranasal administration (P=0.94). A 2-compartment disposition model, with transit intranasal absorption and clearance driven by cardiac output using the well-stirred liver model, was the final PK model. Intranasal bioavailability was estimated to be 40.6% (95% CI 34.7–54.4%) and 40.7% (95% CI 36.5–53.2%) for atomization and drops respectively. Sedation score was modelled via a sigmoidal Emax model driven by an effect compartment. The effect compartment had an equilibration half time 3.3 (95% CI 1.8–4.7) min−1, and the EC50 was estimated to be 903 (95% CI 450–2344) pg ml−1. / Conclusions: There is no difference in bioavailability with atomization or nasal drops. A similar degree of sedation can be achieved by either method. / Clinical trial registration: HKUCTR-1617