Development of chitosan-coated liposome for pulmonary delivery of N-acetylcysteine.

The purpose of the present investigation was to formulate NAC (N-acetylcysteine)-loaded chitosan (CH)-coated liposome aiming at obtaining an effective formulation able to ensure a prolonged and controlled release of NAC to the lung by inhalation. Empty liposomes [(DPPG/Chol/DPPG with different molar percentages of DPPG) (0, 1, 2.5, 5)] were prepared and coated with CH at different CH/Lipid ratio (0.5, 1, 1.5,2, 2.5, W/W) to reach optimum coating of CH. TEM and SEM indicated that morphology of CH-coated and -uncoated liposomes were spherical. FTIR analysis indicated attachment of CH on liposome surface. The drug release experiment in the simulated lung fluid showed that the CH-uncoated and -coated liposomes released 51% and 38% of NAC during 9 h, respectively. The results showed that coating of liposome with CH resulted in the prolonged release of NAC from CH-coated liposome. The results of flow cytometry indicated the effective uptake of CH-coated liposome compared with the CH-uncoated liposome in epithelial cells. In vivo experiment indicated good deposition and retention of CH-coated liposome in lung in comparison with CH-uncoated liposome. The results of the present study demonstrated that CH-coated liposome may represent a promising carrier for the delivery of NAC to the lungs by inhalation therapy.

Enhanced Entrapment and Improved in Vitro Controlled Release of N-Acetyl Cysteine in Hybrid PLGA/Lecithin Nanoparticles Prepared Using a Nanoprecipitation/Self-Assembly Method.

To enhance the in vitro controlled release of N-acetyl cysteine (NAC), hybrid nanoparticles (NPs) consisting of a poly(lactide-co-glycolide) (PLGA) hydrophobic core and a soybean lecithin mono-layer coat were prepared. Hybrid NPs were synthesized using a nanoprecipitation combined with self-assembly method. To characterize prepared NPs, zeta potential, diameter size, surface morphology, disparity, and lipid coating of hybrid NPs were detrmined using dynamic light scattering, scanning electron microscope and Fourier transform infrared spectroscopy techniques. High-performance liquid chromatography was employed to evaluate drug loading yield and encapsulation efficiency and in vitro drug release of prepared NPs. The cytotoxicity of hybrid NPs was assayed on normal L929 alveolar epithelial cells using MTT method. Prepared NPs were found to disperse as individual NPs with a well-defined spherical shape. The hydrodynamic diameter and surface charge of NAC-loaded hybrid NPs were 81.8 ± 1.3 nm and -33.1 ± 2.1 mV, respectively. Drug loading yield and encapsulation efficiency of NAC-loaded hybrid NPs were found to be 38 ± 2.1% and 67 ± 5.7%, respectively. Prepared hybrid NPs showed no significant cytotoxicity against normal alveolar cells. Our data suggest that the hybrid PLGA-lecithin NPs may be An efficient controlled release drug delivery system for NAC. J. Cell. Biochem. 118: 4203-4209, 2017. © 2017 Wiley Periodicals, Inc.

An enquiry on appropriate selection of polymers for preparation of polymeric nanosorbents and nanofiltration/ultrafiltration membranes for hormone micropollutants removal from water effluents.

To analyze polymeric nanosorbents and nanofiltration/ultrafiltration membranes for hormone micropollutants removal from water effluents, here an in-through investigation on the suitability and compatibility of various polymers has been carried out. For this work, estradiol, estrone, testosterone, progesterone, estriol, mestranol, and ethinylestradiol were considered. A total number of 452 polymers were analyzed and initially screened using Hansen solubility parameters. The identified good pairs of hormones and polymers then were examined to obtain the equilibrium capacity of hormones removal from water effluents using a modified Flory-Huggins model. A distribution coefficient was defined as the ratio of hormones in water effluent phase and polymer phase. For removal of mestranol, estradiol and ethinylestradiol, no compatible polymer was identified based on initial screening of collected database. Three compatible polymers were identified for estriol. For progesterone, a wide variety of polymers was identified as good matching of polar, dispersion and hydrogen forces contributions can be observed for these pairs. For estrone, only two polymers can be proposed due to the mismatch observed between polar, dispersion and hydrogen forces contributions of other polymers and this hormone. The phase calculations showed that not all the identified good pairs could be used for practical separation applications. The domain of applicability of each good pair was investigated and potential polymers for practical micropollutants removal together with their removal capacity were represented in terms of phase envelops. The theoretical approach follows fundamental chemical thermodynamic equations and then can be simply applied for any system of interest.

Tat peptide and hexadecylphosphocholine introduction into pegylated liposomal doxorubicin: An in vitro and in vivo study on drug cellular delivery, release, biodistribution and antitumor activity.

We have investigated the co-addition of hexadecylphosphocholine (HePC) and a Tat derived peptide (Tat), coupled to Maleimide-PEG2000-DSPE pegylated liposomal doxorubicin (PLD) in many respects, including drug and liposome cellular delivery, drug release, biodistribution, in vivo cell delivery and antitumor activity. The liposomes were HePC-free and -containing liposomes, from which liposomes with 25, 50, 100 and 200 numbers of Tat/liposome were prepared. Similarly, DiI-C18 (3)-model liposomes (DiI-L and DiI-HePC-L) were prepared. HePC and Tat increased cellular delivery of Dox and cytotoxicity in B16F0 melanoma and C26 colon carcinoma cells. Tat enhanced liposome-cell interaction and caused Dox burst release. HePC and Tat reduced the serum retention time of liposomal Dox, slightly and dramatically, respectively. In comparison, Tat-liposomes enhanced Dox delivery to liver and spleen cells 3h post-injection. Likewise, Dox content of these tissues and tumor was lower at 24h. The naïve liposomes retarded tumor growth more effectively and their related median survival time of the treated C26 bearing BALB/c mice was longer than those of Tat-liposomes (MST>45days versus MST<38days). Overall liposomes exhibiting sustained drug release and negligible cell interaction were more suitable delivery systems in targeting cancerous tumors and suppressing their growth.