Utilization of multilayer-technology to enhance encapsulation efficiency and osmotic gradient tolerance of iron-loaded W1/O/W2 emulsions: Saponin-chitosan coatings

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.

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Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

Current Drug Delivery ◽

10.2174/1567201816666191029125300 ◽

2019 ◽

Vol 16 (10) ◽

pp. 940-950 ◽

Cited By ~ 1

Author(s):

Jiandong Yu ◽

Zhi Chen ◽

Yan-zhi Yin ◽

Chaoyuan Tang ◽

Enying Hu ◽

...

Keyword(s):

Gradient Method ◽

Encapsulation Efficiency ◽

Ph Value ◽

Topical Administration ◽

Ph Gradient ◽

Stability Factor ◽

Buffer Solution ◽

Skin Delivery ◽

Skin Retention

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.

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Microencapsulation ofβ-Carotene by Spray Drying: Effect of Wall Material Concentration and Drying Inlet Temperature

International Journal of Food Science ◽

10.1155/2019/8914852 ◽

2019 ◽

Vol 2019 ◽

pp. 1-12 ◽

Cited By ~ 10

Author(s):

Luiz C. Corrêa-Filho ◽

Maria M. Lourenço ◽

Margarida Moldão-Martins ◽

Vítor D. Alves

Keyword(s):

Antioxidant Activity ◽

Spray Drying ◽

Encapsulation Efficiency ◽

Fruits And Vegetables ◽

Wall Material ◽

Inlet Temperature ◽

Carotene Content ◽

Arabic Gum ◽

Air Inlet ◽

Adverse Environmental Conditions

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.

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OSMOTIC INHIBITION OF THE NATRIFERIC RESPONSE OF THE TOAD URINARY BLADDER TO VASOPRESSIN

Journal of Endocrinology ◽

10.1677/joe.0.0670119 ◽

1975 ◽

Vol 67 (1) ◽

pp. 119-125

Author(s):

P. J. BENTLEY

Keyword(s):

Urinary Bladder ◽

Water Movement ◽

Short Circuit ◽

Electrical Potential ◽

Short Circuit Current ◽

Toad Bladder ◽

Toad Urinary Bladder ◽

Electrical Potential Difference ◽

Osmotic Gradient

SUMMARY The electrical potential difference and short-circuit current (scc, reflecting active transmural sodium transport) across the toad urinary bladder in vitro was unaffected by the presence of hypo-osmotic solutions bathing the mucosal (urinary) surface, providing that the transmural flow of water was small. Vasopressin increased the scc across the toad bladder (the natriferic response), but this stimulation was considerably reduced in the presence of a hypo-osmotic solution on the mucosal side, conditions under which water transfer across the membrane was also increased. This inhibition of the natriferic response did not depend on the direction of the water movement, for if the osmotic gradient was the opposite way to that which normally occurs, the response to vasopressin was still reduced. The natriferic response to cyclic AMP was also inhibited in the presence of an osmotic gradient. Aldosterone increased the scc and Na+ transport across the toad bladder but this response was not changed when an osmotic gradient was present. The physiological implications of these observations and the possible mechanisms involved are discussed.

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Preparation of Artificial Red Blood Cells (Hemoglobin Vesicles) Using the Rotation–Revolution Mixer for High Encapsulation Efficiency

ACS Biomaterials Science & Engineering ◽

10.1021/acsbiomaterials.1c00424 ◽

2021 ◽

Author(s):

Tomoko Kure ◽

Hiromi Sakai

Keyword(s):

Red Blood Cells ◽

Blood Cells ◽

Encapsulation Efficiency

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Ultrasonic cavitation driven fabrication of organic solvent free lignin/prochloraz nano capsules to promote resistance to photolysis and rain wash, and provide extended release performance

Holzforschung ◽

10.1515/hf-2020-0120 ◽

2021 ◽

Vol 0 (0) ◽

Author(s):

Jingtian Chen ◽

Miao Wang ◽

Yong Qian ◽

Shanyuan Tan ◽

Huan Wang ◽

...

Keyword(s):

Organic Solvent ◽

Uv Irradiation ◽

Encapsulation Efficiency ◽

Extended Release ◽

Ultrasonic Cavitation ◽

Solvent Free ◽

Loading Capacity ◽

One Pot ◽

Continuous Release ◽

Mango Leaves

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.

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Mixing Oil-Based Microencapsulation of Garlic Essential Oil: Impact of Incorporating Three Commercial Vegetable Oils on the Stability of Emulsions

Foods ◽

10.3390/foods10071637 ◽

2021 ◽

Vol 10 (7) ◽

pp. 1637

Author(s):

Yunjiao Zhao ◽

Rui Liu ◽

Cuiping Qi ◽

Wen Li ◽

Mohamed Rifky ◽

...

Keyword(s):

Essential Oil ◽

Vegetable Oils ◽

Encapsulation Efficiency ◽

Ostwald Ripening ◽

Corn Oil ◽

Whey Protein Concentrate ◽

Diallyl Disulfide ◽

Active Components ◽

The Stability ◽

Garlic Essential Oil

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.

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Delivery of melittin-loaded niosomes for breast cancer treatment: an in vitro and in vivo evaluation of anti-cancer effect

Cancer Nanotechnology ◽

10.1186/s12645-021-00085-9 ◽

2021 ◽

Vol 12 (1) ◽

Author(s):

Farnaz Dabbagh Moghaddam ◽

Iman Akbarzadeh ◽

Ehsan Marzbankia ◽

Mahsa Farid ◽

Leila khaledi ◽

...

Keyword(s):

Breast Cancer ◽

Cancer Treatment ◽

Cell Lines ◽

Encapsulation Efficiency ◽

Inbred Mice ◽

Breast Cancer Treatment ◽

Anticancer Effect ◽

Anti Cancer

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.

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