Niosomes (the nonionic surfactant vesicles), considered as novel drug delivery systems, can improve the solubility and stability of natural pharmaceutical molecules. They are established to provide targeting and controlled release of natural pharmaceutical compounds. Many factors can influence on niosome construction such as the preparation method, type and amount of surfactant, drug entrapment, temperature of lipids hydration, and the packing factor. The present review discusses about the most important features of niosomes such as their diverse structures, the different preparation approaches, characterization techniques, factors that affect their stability, their use by various routes of administration, their therapeutic applications in comparison with natural drugs, and specially the brain targeting with niosomes-ligand conjugation. It also provides recent data about the various types of ligand agents which make available active targeting drug delivery to the central neuron system. This system has an optimistic upcoming in pharmaceutical uses, mostly with the improving availability of innovative schemes to overcome blood-brain barrier and targeting the niosomes to the brain.

Purpose: Among the potent anticancer agents, d,l-sulforaphane (SF) is very effective against many different types of cancer cells. Its clinical application is restricted because of its hydrophobicity, low gastrointestinal absorption and poor bioavailability. In the present study, a reliable micellar delivery system using monomethoxypoly (ethylene glycol)–poly (ɛ-caprolactone) (mPEG–PCL) was established. The encapsulation of SF inside mPEG–PCL as a nano-carrier was established and the cytotoxicity assay against human breast cancer cell line was evaluated. Methods: In this study, SF was encapsulated within mPEG–PCL micelles through a single-step nano-precipitation method, leading to creation of SF-loaded mPEG–PCL (SF/mPEG–PCL) micelles. Di-block mPEG–PCL copolymers were synthesized and used to prepare micelles. MPEG-PCL copolymer was characterized by HNMR, FTIR, differential scanning calorimetry and gel permeation chromatography techniques. Characterization, stability of micelles, the particle size and morphology were determined. The release profile of the SF from the micelles which prepared by the drug-loaded copolymer, was evaluated. The cytotoxicity of free SF, mPEG–PCL and SF-loaded mPEG–PCL micelles was compared with each other by performing MTT assay of the treated MCF-7 cell line. Expression levels of BCL-2, MMP-9, BCL-XL, BAK, BAX and GAPDH (endogenous gene) as control were quantified by real time PCR. To evaluate the apoptotic effects of Free SF compared with SF-loaded mPEG–PCL micelles, flow cytometry analysis was done using the annexin V-FITC apoptosis detection kit. Results: Our studies resulted in a successful establishment of uniformity and spherical SF-loaded mPEG–PCL micelles. The encapsulation efficiency of SF was 86 ± 1.58%. The results of atomic force microscopy revealed that the micelles have spherical shapes with size of 107 nm. In vitro release of SF from SF-entrapped micelles was remarkably sustained. The mPEG–PCL micelle showed little cytotoxicity in the case of MCF-7 cell line with concentration up to 1.5 mg/ml, whereas the SF-loaded mPEG–PCL micelles at all concentrations significantly was cytotoxic in the case of MCF-7 cell line. Finally, real-time PCR and flow cytometry were used to demonstrate that the SF-loaded mPEG–PCL could be efficiently inducing apoptosis in MCF-7 cell line. Conclusion: We achieved to a successful formulation of SF-loaded m-PEG/PCL micelles in this study. Based on the cytotoxicity results of mPEG–PCL micelles against human breast cancer cell line (MCF-7) in this study, it suggested that SF/mPEG–PCL micelles can be an effective breast cancer treatment strategy in the future.

Among the potent anticancer agents, curcumin is known as an effective agent against many different types of cancer cells. Its clinical applications have been limited because of hydrophobicity, low gastrointestinal absorption and fast metabolism. In the present study, curcumin was encapsulated within PCL–PEG–PCL micelles through a single-step nano-precipitation method, leading to the creation of CUR/PCL–PEG–PCL micelles. The PCL–PEG–PCL copolymer was characterized in vitro using ¹H NMR, FTIR, DSC and GPC techniques. PCL–PEG–PCL copolymers with curcumin were self-assembled into micelles in aqueous solution. The resulting micelles were characterized further using various techniques such as DLS and AFM. The anti-tumor properties of curcumin-loaded micelles were evaluated in cancer cell lines both in vitro and in vivo. The results showed the successful formation of spherical curcumin-loaded micelles. The encapsulation efficiency of curcumin was 83 ± 1.29%. The results of AFM revealed that the micelles have spherical shapes with a size of 70.34 nm. In vitro release of curcumin from curcumin-entrapped micelles followed a remarkably sustained release profile. The curcumin-loaded micelle showed an efficient physical stability and a high loading efficiency. The results of in vivo experiments indicated that the curcumin-loaded micelles significantly reduce the tumor size, prolong the survival and increase splenocyte proliferation and IFN-γ production as well as significantly decreasing the IL-4 production. The results indicate that the successful formulation of curcumin loaded PCL–PEG–PCL micelles had a significant chemopreventive effect on cancer cell lines through cell proliferation inhibition, apoptosis induction and anti-tumor immunity stimulation.