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| 1 | Liposomal remdesivir inhalation solution for targeted lung delivery as a novel therapeutic approach for COVID-19显示文摘Strong infectivity enables coronavirus disease 2019(COVID-19)to rage throughout the world.Moreover,the lack of drugs with definite therapeutic effects further aggravates the spread of the pandemic.Remdesivir is one of the most promising anti-severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)drugs.However,the limited clinical effects make its therapeutic effect controversial,which may result from the poor accumulation and activation of remdesivir in the lung.Therefore,we developed lyophilized remdesivir liposomes(Rdv-lips)which can be reconstituted as liposomal aerosol for pulmonary delivery to improve the in vivo behavior of existing remdesivir cyclodextrin conclusion compound(Rdv-cyc)injections.Liposome encapsulation endowed remdesivir with much higher solubility and better biocompatibility.The in vitro liposomal aerosol characterization demonstrated that Rdv-lips possessed a mass median aerodynamic diameter of 4.118μm and fine particle fraction(<5μm)higher than 50%,indicating good pulmonary delivery properties.Compared to the Rdv-cyc intravenous injection group,the Rdv-lips inhalation group displayed a nearly 100-fold increase in the remdesivir-active metabolite nucleotide triphosphate(NTP)concentration and better NTP accumulation in the lung than the Rdv-cyc inhalation group.A faster transition from remdesivir to NTP of Rdv-lips(inhalation)could also be observed due to better cell uptake.Compared to other preparations,the superiority of Rdv-lips was further evidenced by the results of an in vivo safety study,with little possibility of inducing inflammation.In conclusion,Rdv-lips for pulmonary delivery will be a potent formulation to improve the in vivo behavior of remdesivir and exert better therapeutic effects in COVID-19 treatment. | Jingjing Li Kai Zhang Di Wua Lianjie Ren Xinyu Chu Chao Qin Xiaopeng Han Taijun Hang Yungen Xu Lei Yang Lifang Yina | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，6： | 0 |
| 2 | Microspheres as pulmonary delivery systems-A review显示文摘Microspheres are one of the delivery systems,which can be used to protect drugs or proteins especially for pulmonary purposes since these particles can be a direct target to the lung and their mucoadhesive properties.Their advantages could help cure pulmonary diseases.There are several methods of polymers to form microspheres depending on the physicochemical characteristics of polymers.In this review,we aimed to discuss methods to produce microspheres from conventional to advanced techniques,and various polymers that can be designed to form microspheres,and aerosolization properties of the inhalable particles for pulmonary delivery were discussed.With this comprehensive review,our findings will enhance pharmaceutical knowledge,promote wide uses of microspheres,and produce new techniques to prepare inhalable pulmonary microspheres. | Dewi Melani Hariyadi Esti Hendradi Herlina Eka Pratama Mahardian Rahmadi | 2021 | Journal of Chinese Pharmaceutical Sciences2021，30，7： | 0 |
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