The major challenge faced by today's pharmacologist and formulation scientist is ocular drug delivery. Topical eye drop is the most convenient and patient compliant route of drug administration,especially for the ...The major challenge faced by today's pharmacologist and formulation scientist is ocular drug delivery. Topical eye drop is the most convenient and patient compliant route of drug administration,especially for the treatment of anterior segment diseases. Delivery of drugs to the targeted ocular tissues is restricted by various precorneal,dynamic and static ocular barriers. Also,therapeutic drug levels are not maintained for longer duration in target tissues. In the past two decades,ocular drug delivery research acceleratedly advanced towards developing a novel,safe and patient compliant formulation and drug delivery devices/techniques,which may surpass these barriers and maintain drug levels in tissues. Anterior segment drug delivery advances are witnessed by modulation of conventional topical solutions with permeation and viscosity enhancers. Also,it includes development of conventional topical formulations such as suspensions,emulsions and ointments. Various nanoformulations have also been introduced for anterior segment ocular drug delivery. On the other hand,for posterior ocular delivery,research has been immensely focused towards development of drug releasing devices and nanoformulations for treating chronic vitreo-retinal diseases. These novel devices and/or formulations may help to surpass ocular barriers and associated side effects with conventional topicaldrops. Also,these novel devices and/or formulations are easy to formulate,no/negligibly irritating,possess high precorneal residence time,sustain the drug release,and enhance ocular bioavailability of therapeutics. An update of current research advancement in ocular drug delivery necessitates and helps drug delivery scientists to modulate their think process and develop novel and safe drug delivery strategies. Current review intends to summarize the existing conventional formulations for ocular delivery and their advancements followed by current nanotechnology based formulation developments. Also,recent developments with other ocular drug delivery strateg展开更多
Hepatic fibrosis is one kind of liver diseases with a high mortality rate and incidence.The activation and proliferation of hepatic stellate cells(HSCs)is the most fundamental reason of hepatic fibrosis.There are no s...Hepatic fibrosis is one kind of liver diseases with a high mortality rate and incidence.The activation and proliferation of hepatic stellate cells(HSCs)is the most fundamental reason of hepatic fibrosis.There are no specific and effective drug delivery carriers for the treatment of hepatic fibrosis at present.We found that when hepatic fibrosis occurs,the expression of CD44 receptors on the surface of HSCs is significantly increased.Based on this finding,we designed silibinin-loaded hyaluronic acid(SLB-HA)micelles to achieve the treatment of hepatic fibrosis.Meanwhile,we constructed liver fibrosis rat model using Sprague-Dawley rats.We demonstrated that HA micelles had specific uptake to HSCs in vitro while avoiding the distribution in normal liver cells and the phagocytosis of macrophages.Importantly,HA micelles showed a significant liver targeting effect in vivo,especially in fibrotic liver which highly expressed CD44 receptors.In addition,SLB-HA micelles could selectively kill activated HSCs,having an excellent anti-hepatic fibrosis effect in vivo and a significant sustained release effect,and also had a good biological safety and biocompatibility.Overall,HA micelles represented a novel nanomicelle system which showed great potentiality in anti-hepatic fibrosis drugs delivery.展开更多
文摘The major challenge faced by today's pharmacologist and formulation scientist is ocular drug delivery. Topical eye drop is the most convenient and patient compliant route of drug administration,especially for the treatment of anterior segment diseases. Delivery of drugs to the targeted ocular tissues is restricted by various precorneal,dynamic and static ocular barriers. Also,therapeutic drug levels are not maintained for longer duration in target tissues. In the past two decades,ocular drug delivery research acceleratedly advanced towards developing a novel,safe and patient compliant formulation and drug delivery devices/techniques,which may surpass these barriers and maintain drug levels in tissues. Anterior segment drug delivery advances are witnessed by modulation of conventional topical solutions with permeation and viscosity enhancers. Also,it includes development of conventional topical formulations such as suspensions,emulsions and ointments. Various nanoformulations have also been introduced for anterior segment ocular drug delivery. On the other hand,for posterior ocular delivery,research has been immensely focused towards development of drug releasing devices and nanoformulations for treating chronic vitreo-retinal diseases. These novel devices and/or formulations may help to surpass ocular barriers and associated side effects with conventional topicaldrops. Also,these novel devices and/or formulations are easy to formulate,no/negligibly irritating,possess high precorneal residence time,sustain the drug release,and enhance ocular bioavailability of therapeutics. An update of current research advancement in ocular drug delivery necessitates and helps drug delivery scientists to modulate their think process and develop novel and safe drug delivery strategies. Current review intends to summarize the existing conventional formulations for ocular delivery and their advancements followed by current nanotechnology based formulation developments. Also,recent developments with other ocular drug delivery strateg
基金financially supported by National Natural Science Foundation of China(81673359)Sichuan Major Science and Technology Project on Biotechnology and Medicine(No.2018SZDZX0018,China).
文摘Hepatic fibrosis is one kind of liver diseases with a high mortality rate and incidence.The activation and proliferation of hepatic stellate cells(HSCs)is the most fundamental reason of hepatic fibrosis.There are no specific and effective drug delivery carriers for the treatment of hepatic fibrosis at present.We found that when hepatic fibrosis occurs,the expression of CD44 receptors on the surface of HSCs is significantly increased.Based on this finding,we designed silibinin-loaded hyaluronic acid(SLB-HA)micelles to achieve the treatment of hepatic fibrosis.Meanwhile,we constructed liver fibrosis rat model using Sprague-Dawley rats.We demonstrated that HA micelles had specific uptake to HSCs in vitro while avoiding the distribution in normal liver cells and the phagocytosis of macrophages.Importantly,HA micelles showed a significant liver targeting effect in vivo,especially in fibrotic liver which highly expressed CD44 receptors.In addition,SLB-HA micelles could selectively kill activated HSCs,having an excellent anti-hepatic fibrosis effect in vivo and a significant sustained release effect,and also had a good biological safety and biocompatibility.Overall,HA micelles represented a novel nanomicelle system which showed great potentiality in anti-hepatic fibrosis drugs delivery.
