RNA interference(RNAi)using small interfering RNA(siRNA)has shown potential as a therapeutic option for the treatment of arthritis by silencing specific genes.However,siRNA delivery faces several challenges,including ...RNA interference(RNAi)using small interfering RNA(siRNA)has shown potential as a therapeutic option for the treatment of arthritis by silencing specific genes.However,siRNA delivery faces several challenges,including stability,targeting,off-target effects,endosomal escape,immune response activation,intravascular degradation,and renal clearance.A variety of nanotherapeutics like lipidic nanoparticles,liposomes,polymeric nanoparticles,and solid lipid nanoparticles have been developed to improve siRNA cellular uptake,protect it from degradation,and enhance its therapeutic efficacy.Researchers are also investigating chemical modifications and bioconjugation to reduce its immunogenicity.This review discusses the potential of siRNA nanotherapeutics as a therapeutic option for various immune-mediated diseases,including rheumatoid arthritis,osteoarthritis,etc.siRNA nanotherapeutics have shown an upsurge of interest and the future looks promising for such interdisciplinary approach-based modalities that combine the principles of molecular biology,nanotechnology,and formulation sciences.展开更多
Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of...Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of atorvasta tin was prepared by lyophilization utilising skimmed milk as a carrier.Six different formulations were prepared with varying ratios of drug and carrier and the corresponding physical mixtures were also prepared.The formation of a solid dispersion formulation was confirmed by differential scanning ca lorimetry and X-ray diffraction studies.The optimum drug-to-carrier ratio of 1:9 en hanced solubility nearly 33-fold as compared to pure drug.In vitro drug release studies exhibited a cumulative release of 83.69% as compared to 22.7% for the pure drug.Additionally,scanning electron microscopy studies suggested the conversion of crystalline atorvastatin to an amorphous form.In a Triton-induced hyperlipidemia model,a 3-fold increase in the lipid lowering potential was obtained with the reformulated drug as compared to pure drug.These results suggest that solid dispersion of atorvastatin using skimmed milk as carrier is a promising approach for oral delivery of atorvastatin.展开更多
文摘RNA interference(RNAi)using small interfering RNA(siRNA)has shown potential as a therapeutic option for the treatment of arthritis by silencing specific genes.However,siRNA delivery faces several challenges,including stability,targeting,off-target effects,endosomal escape,immune response activation,intravascular degradation,and renal clearance.A variety of nanotherapeutics like lipidic nanoparticles,liposomes,polymeric nanoparticles,and solid lipid nanoparticles have been developed to improve siRNA cellular uptake,protect it from degradation,and enhance its therapeutic efficacy.Researchers are also investigating chemical modifications and bioconjugation to reduce its immunogenicity.This review discusses the potential of siRNA nanotherapeutics as a therapeutic option for various immune-mediated diseases,including rheumatoid arthritis,osteoarthritis,etc.siRNA nanotherapeutics have shown an upsurge of interest and the future looks promising for such interdisciplinary approach-based modalities that combine the principles of molecular biology,nanotechnology,and formulation sciences.
文摘Atorvastatin has low aqueous solubility resulting in low oral bioavailability(12%)and thus presents a challenge in formulating a suitable dosage form.To improve the aqueous solubility,a solid dispersion formulation of atorvasta tin was prepared by lyophilization utilising skimmed milk as a carrier.Six different formulations were prepared with varying ratios of drug and carrier and the corresponding physical mixtures were also prepared.The formation of a solid dispersion formulation was confirmed by differential scanning ca lorimetry and X-ray diffraction studies.The optimum drug-to-carrier ratio of 1:9 en hanced solubility nearly 33-fold as compared to pure drug.In vitro drug release studies exhibited a cumulative release of 83.69% as compared to 22.7% for the pure drug.Additionally,scanning electron microscopy studies suggested the conversion of crystalline atorvastatin to an amorphous form.In a Triton-induced hyperlipidemia model,a 3-fold increase in the lipid lowering potential was obtained with the reformulated drug as compared to pure drug.These results suggest that solid dispersion of atorvastatin using skimmed milk as carrier is a promising approach for oral delivery of atorvastatin.