End-chain fluorination of polyesters favors perfluorooctyl bromide encapsulation into echogenic PEGylated nanocapsules

2017 ◽  
Vol 8 (16) ◽  
pp. 2559-2570 ◽  
Author(s):  
Sophie Houvenagel ◽  
Guilherme Picheth ◽  
Camille Dejean ◽  
Annie Brûlet ◽  
Alexis Chennevière ◽  
...  

Fluorination of polyesters favors the encapsulation efficiency of perfluorooctyl bromide into nanocapsules.


2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.



2019 ◽  
Vol 16 (10) ◽  
pp. 940-950 ◽  
Author(s):  
Jiandong Yu ◽  
Zhi Chen ◽  
Yan-zhi Yin ◽  
Chaoyuan Tang ◽  
Enying Hu ◽  
...  

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.



2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Luiz C. Corrêa-Filho ◽  
Maria M. Lourenço ◽  
Margarida Moldão-Martins ◽  
Vítor D. Alves

Carotenoids are a class of natural pigments found mainly in fruits and vegetables. Among them,β-carotene is regarded the most potent precursor of vitamin A. However, it is susceptible to oxidation upon exposure to oxygen, light, and heat, which can result in loss of colour, antioxidant activity, and vitamin activity. Thus, the objective of this work was to study the microencapsulation process ofβ-carotene by spray drying, using arabic gum as wall material, to protect it against adverse environmental conditions. This was carried out using the response surface methodology coupled to a central composite rotatable design, evaluating simultaneously the effect of drying air inlet temperature (110-200°C) and the wall material concentration (5-35%) on the drying yield, encapsulation efficiency, loading capacity, and antioxidant activity. In addition, morphology and particles size distribution were evaluated. Scanning electron microscopy images have shown that the particles were microcapsules with a smooth surface when produced at the higher drying temperatures tested, most of them having a diameter lower than 10μm. The conditions that enabled obtaining simultaneously arabic gum microparticles with higherβ-carotene content, higher encapsulation efficiency, and higher drying yield were a wall material concentration of 11.9% and a drying inlet temperature of 173°C. The systematic approach used for the study ofβ-carotene microencapsulation process by spray drying using arabic gum may be easily applied for other core and wall materials.



Holzforschung ◽  
2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Jingtian Chen ◽  
Miao Wang ◽  
Yong Qian ◽  
Shanyuan Tan ◽  
Huan Wang ◽  
...  

Abstract Lignin is a natural macromolecular sun blocker and provides an ideal protection material for pesticides that have poor photostability. In this study, alkali lignin/prochloraz capsules (AL-P) were prepared via one-pot ultrasonic cavitation. The results demonstrated that the produced AL-P were uniform spheres with sizes of 170–375 nm. The prochloraz encapsulation efficiency (EE) and loading capacity (LC) reached as high as 91.8 and 98.5%, respectively. Adding a small of surfactant reduced the size of the capsules, but both EE and LC were decreased. AL-P exhibited excellent extended release performance. The cumulative release of AL-P in the first 45 h was 76.1% and continuous release was maintained after 96 h. The resulting AL-P have improved photostability under UV irradiation radiation. Finally, AL-P capsules were sprayed on the mango leaves and bananas to act as preservatives, AL-P capsules had stronger rain wash resistance and were better preserved demonstrating their industrial applicability. Together, organic solvent free AL-P capsules demonstrate a method to improve the efficiency of photosensitive pesticides.



Foods ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1637
Author(s):  
Yunjiao Zhao ◽  
Rui Liu ◽  
Cuiping Qi ◽  
Wen Li ◽  
Mohamed Rifky ◽  
...  

The active components in garlic essential oil are easily degradable, which limits its application in the food industry. Vegetable oils (VOs) were used to improve the stability of garlic essential oil (GEO) emulsion. The volatile compounds of GEO and its mixtures with vegetable oils (VOs), including corn oil (CO), soybean oil (SO), and olive oil (OO) indicated that GEO-VO mixtures had a higher percentage of Diallyl disulfide and Diallyl trisulfide than pure GEO. Adding an appropriate amount of VOs promoted the GEO emulsion (whey protein concentrate and inulin as the wall materials) stability in order of CO > SO > OO. Evaluation of the encapsulation efficiency, controlled release, and antimicrobial activity of GEO-VO microcapsules showed that the GEO was successfully entrapped and slowly released with active antibacterial activities on both E. coli and S. aureus. Collectively, these results implied that VOs, especially for 20% CO, improved the stability of GEO emulsions and the encapsulation efficiency of GEO microcapsules. The mechanism might be related to (1) the regulating effect of density difference between oil and water phases on prevention to gravitational separation, (2) the promotion to the compatibility of GEO and VOs to inhibit the phase separation caused by Ostwald ripening.



2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Farnaz Dabbagh Moghaddam ◽  
Iman Akbarzadeh ◽  
Ehsan Marzbankia ◽  
Mahsa Farid ◽  
Leila khaledi ◽  
...  

Abstract Background Melittin, a peptide component of honey bee venom, is an appealing candidate for cancer therapy. In the current study, melittin, melittin-loaded niosome, and empty niosome had been optimized and the anticancer effect assessed in vitro on 4T1 and SKBR3 breast cell lines and in vivo on BALB/C inbred mice. "Thin-layer hydration method" was used for preparing the niosomes; different niosomal formulations of melittin were prepared and characterized in terms of morphology, size, polydispersity index, encapsulation efficiency, release kinetics, and stability. A niosome was formulated and loaded with melittin as a promising drug carrier system for chemotherapy of the breast cancer cells. Hemolysis, apoptosis, cell cytotoxicity, invasion and migration of selected concentrations of melittin, and melittin-loaded niosome were evaluated on 4T1 and SKBR3 cells using hemolytic activity assay, flow cytometry, MTT assay, soft agar colony assay, and wound healing assay. Real-time PCR was used to determine the gene expression. 40 BALB/c inbred mice were used; then, the histopathology, P53 immunohistochemical assay and estimate of renal and liver enzyme activity for all groups had been done. Results This study showed melittin-loaded niosome is an excellent substitute in breast cancer treatment due to enhanced targeting, encapsulation efficiency, PDI, and release rate and shows a high anticancer effect on cell lines. The melittin-loaded niosome affects the genes expression by studied cells were higher than other samples; down-regulates the expression of Bcl2, MMP2, and MMP9 genes while they up-regulate the expression of Bax, Caspase3 and Caspase9 genes. They have also enhanced the apoptosis rate and inhibited cell migration, invasion in both cell lines compared to the melittin samples. Results of histopathology showed reduce mitosis index, invasion and pleomorphism in melittin-loaded niosome. Renal and hepatic biomarker activity did not significantly differ in melittin-loaded niosome and melittin compared to healthy control. In immunohistochemistry, P53 expression did not show a significant change in all groups. Conclusions Our study successfully declares that melittin-loaded niosome had more anti-cancer effects than free melittin. This project has demonstrated that niosomes are suitable vesicle carriers for melittin, compare to the free form.



Nanoscale ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 5410-5418
Author(s):  
Rocío López-Cabeza ◽  
Melanie Kah ◽  
Renato Grillo ◽  
Zuzana Bílková ◽  
Jakub Hofman

Encapsulation efficiency of nanoformulated pesticides is often determined by centrifugal ultrafiltration.



LWT ◽  
2021 ◽  
pp. 111430
Author(s):  
Xiao Wang ◽  
Zhuang Ding ◽  
Yanna Zhao ◽  
Sangeeta Prakash ◽  
Wenlai Liu ◽  
...  


Life ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 223
Author(s):  
Boying Xu ◽  
Jinquan Ding ◽  
Jian Xu ◽  
Tetsuya Yomo

(1) Background: giant vesicles (GVs) are widely employed as models for studying physicochemical properties of bio-membranes and artificial cell construction due to their similarities to natural cell membranes. Considering the critical roles of GVs, various methods have been developed to prepare them. Notably, the water-in-oil (w/o) inverted emulsion-transfer method is reported to be the most promising, owning to the relatively higher productivity and better encapsulation efficiency of biomolecules. Previously, we successfully established an improved approach to acquire detailed information of 1-Palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC)-derived GVs with imaging flow cytometry (IFC); (2) Methods: we prepared GVs with different lipid compositions, including phosphatidylcholines (PCs), phosphatidylethanolamines (PEs), and PC/PE mixtures by w/o inverted emulsion methods. We comprehensively compared the yield, purity, size, and encapsulation efficiency of the resulting vesicles; (3) Results: the relatively higher productivities of GVs could be obtained from POPC, 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1,2-dilauroyl-sn-glycero-3-phosphoethanolamine (DLPE), DOPC: DLPE (7:3), and POPC: DLPE (6:4) pools. Furthermore, we also demonstrate that these GVs are stable during long term preservation in 4 °C. (4) Conclusions: our results will be useful for the analytical study of GVs and GV-based applications.



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