scholarly journals Preparation of Folic Acid-conjugated Albumin Nanoparticles Containing Paclitaxel using High-pressure Homogenisation Coagulation Method

Author(s):  
Yan Chu ◽  
Shuo Chai ◽  
Hong Pan ◽  
Jiayi Qian ◽  
Cuiyan Han ◽  
...  

Abstract In this study, we prepared and evaluated folic acid-conjugated albumin-paclitaxel (FA-BSA-PTX) nanoparticles using a new green technique, called the high-pressure homogenisation coagulation method (HPHCM). The effect of process parameters such as BSA concentration, coagulant concentration, homogenisation time, homogenisation pressure, water/ethanol ratio, and BSA/PTX ratio was analysed to optimise nanoparticle size, albumin conversion rate, and encapsulation efficiency. BSA concentration was found to exert a great influence on albumin conversion rate and particle size. Meanwhile, the BSA/PTX ratio significantly affected the nanoparticle encapsulation efficiency. Electron microscopy showed that the freeze-dried particles mostly existed in the form of dimers and trimers with an average particle size of 300–400 nm. Infrared spectroscopy indicated that PTX was well encapsulated in BSA. Raman spectra of the synthesised nanoparticles indicated changes in the disulphide bond configuration and protein structure. In vitro drug-release analysis showed that crosslinked nanoparticles exhibited a sustained release. Furthermore, in vitro cell-uptake studies on HeLa cells showed that FA can be used as a targeting ligand for albumin carriers to enhance the active targeting effect of the nanoparticles with a high FR expression. These results suggest that HPHCM is an effective method to prepare FA-BSA-PTX drug-delivery systems.

Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.


Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 23
Author(s):  
Hua-Wei Chen ◽  
Yu-Wei Chang ◽  
Wu-Po Fang

Toxic organic solvent residues and the active substances of thermal degradation (such as anthocyanin and polyphenols) are always a concern with the liposomes produced by traditional techniques. The present study focuses on a new approach for the microencapsulation of Clitoria ternatea petal (CTP) extracts, which contain anthocyanins, by high-pressure processing (HPP) at room temperature. Thus, a series of CTP liposomes were prepared and their physicochemical properties were analyzed by laser granulometry and by scanning electron microscopy (SEM). The results revealed that the average particle size of the liposomes after HPP treatment increased gradually from 300 MPa to 600 MPa, possibly due to the aggregation of liposomes and damage to the phospholipid bilayers. For the preparation of liposomes by the HPP method at 300 MPa, the mean particle size, polydispersity index (PDI), and encapsulation efficiency were 240.7 nm, 0.37, and 77.8%, respectively. The HPP method provided a number of advantages over conventional methods (magnet stirring and ultrasonication) as it could allow liposome preparation with higher encapsulation efficiency, smaller size, and narrower, more reproducible particle size distribution. Conclusively, microencapsulation in the liposomes was successfully achieved with the fast-adiabatic expansion of HPP.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
K. A. Athmaselvi ◽  
C. Kumar ◽  
M. Balasubramanian ◽  
Ishita Roy

This study evaluates the physical properties of freeze dried tropical (guava, sapota, and papaya) fruit powders. Thermal stability and weight loss were evaluated using TGA-DSC and IR, which showed pectin as the main solid constituent. LCR meter measured electrical conductivity, dielectric constant, and dielectric loss factor. Functional groups assessed by FTIR showed presence of chlorides, and O–H and N–H bonds in guava, chloride and C–H bond in papaya, and chlorides, and C=O and C–H bonds in sapota. Particle size and type of starch were evaluated by X-ray diffraction and microstructure through scanning electronic microscopy. A semicrystalline profile and average particle size of the fruit powders were evidenced by X-ray diffraction and lamellar/spherical morphologies by SEM. Presence of A-type starch was observed in all three fruits. Dependence of electric and dielectric properties on frequency and temperature was observed.


2022 ◽  
Vol 8 ◽  
Author(s):  
Ao Li ◽  
Aixia Zhu ◽  
Di Kong ◽  
Chunwei Wang ◽  
Shiping Liu ◽  
...  

For improving solubility and bioaccessibility of phytosterols (PS), phytosterol nanoparticles (PNPs) were prepared by emulsification–evaporation combined high-pressure homogenization method. The organic phase was formed with the dissolved PS and soybean lecithin (SL) in anhydrous ethanol, then mixed with soy protein isolate (SPI) solution, and homogenized into nanoparticles, followed by the evaporation of ethanol. The optimum fabrication conditions were determined as PS (1%, w/v): SL of 1:4, SPI content of 0.75% (w/v), and ethanol volume of 16 ml. PNPs were characterized to have average particle size 93.35 nm, polydispersity index (PDI) 0.179, zeta potential −29.3 mV, and encapsulation efficiency (EE) 97.3%. The impact of temperature, pH, and ionic strength on the stability of fabricated PNPs was determined. After 3-h in vitro digestion, the bioaccessibility of PS in nanoparticles reached 70.8%, significantly higher than the 18.2% of raw PS. Upon freeze-drying, the particle size of PNPs increased to 199.1 nm, resulting in a bimodal distribution. The solubility of PS in water could reach up to 2.122 mg/ml, ~155 times higher than that of raw PS. Therefore, this study contributes to the development of functional PS-food ingredients.


Author(s):  
Mohammed Sabar Al-lami ◽  
Malath H. Oudah ◽  
Firas A. Rahi

This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formula was obtained with lowest average particle size of 84.05. This formula was studied for compatibility by FTIR and DSC, surface morphology by FESEM and crystalline state by XRPD. Then domperidone nanoparticles were formulated into a simple capsule dosage form in order to study of the in vitro release of drug from nanoparticles in comparison raw drug and mixture of polymer:drug ratios of 2:1. The release of domperidone from best formula was highly improved with a significant (p? 0.05) increase.


2021 ◽  
Vol 10 ◽  
Author(s):  
Venkata Subbaiah Kotakadi ◽  
Bhulakshmi Kolapalli ◽  
Susmila Aparna Gaddam ◽  
Sai Gopal Divi Venkata Ramana

Background: There is an increasing commercial demand for nanoparticles due to their wide applicability in various areas such as chemistry, catalysis, energy and medicine. Metallic nanoparticles are traditionally synthesized by wet chemical techniques where the chemicals used are quite often toxic and flammable. Objective: In the present study, we described a simple, cost effective and environmentally-friendly technique for green synthesis of silver and iron nanoparticles by using the aqueous extract of leafy vegetable Amaranthus viridis as a reducing agent. Methods: The silver and Iron nanoparticles (Av-AgNPs, Av-IONPs) were characterized by different spectral methods. The surface Plasmon resonance spectrums of Av-AgNPs, Av-IONPs were recorded at 422nm and 261nm. The Scanning electron microscopy (SEM) analysis reveals that the Av-AgNPs, Av-IONPs are roughly spherical in shape. Energy dispersive absorption spectroscopy (EDAX) of biosynthesized Av-AgNPs, Av-IONPs indicates the reduction of silver ions to elemental silver and iron ions to elemental iron. Results: The particle size analysis of Av-AgNPs and Av-IONPs was carried out by Dynamic light scattering (DLS) method the results reveal that both Av-AgNPs and Av-IONPs were polydispered in nature. The average particle size of Av-AgNPs is 55.8 nm with a polydispered index (PI) of 0.297, similarly the average particle size of Av-IONPs is 80.6 nm with an polydispered index (PI) of 0.469. Zeta-potential of Av-AgNPs was detected at -24.6 mV and Av-IONPs were detected at 28.8 mV, the result reveals that they high stability due their high negative charge and positive charge respectively. The dual synthesized Av-AgNPs, Av-IONPs exhibits excellent antioxidant activity by DPPH, H2O2 and NO methods. DPPH was proven to be the best when compared with the other two methods. The biosynthesized Av-AgNPs, Av-IONPs proved to have very good antimicrobial activity against gram +ve and gram –ve bacteria. Conclusion: when compared with standard antibiotic. There were several reports on green synthesis of metal nanoparticles using various plant parts, but here edible leafy vegetable Amaranthus viridis was used for biosynthesis of both Av-AgNPs and Av-IONPs.


2019 ◽  
Vol 99 (4) ◽  
pp. 713-723 ◽  
Author(s):  
Gabriela Tasso Pinheiro Machado ◽  
Maria Beatriz Veleirinho ◽  
Letícia Mazzarino ◽  
Luiz Carlos Pinheiro Machado Filho ◽  
Marcelo Maraschin ◽  
...  

This study describes the development of propolis nanoparticles (PNP) to treat bovine mastitis. Three PNP prepared with varying concentrations of propolis (5% and 7%, w/v) and the surfactants [poloxamer (1%, 3%, and 4%, w/v) and soy lecithin (0.25%, 0.7%, and 1%, w/v)]. PNP were characterized according to their size, polydispersity, zeta potential, pH, morphology, and physical stability. PNP were evaluated for their in vitro antimicrobial and cytotoxic effects. PNP obtained were spherical with a monodisperse distribution (polydispersity index < 0.2) and an average particle size between 181 and 201 nm. Stability studies showed that PNP were stable over 150 d. The encapsulation efficiency of total phenolic content varied between 73% and 91%. The chromatographic profile of phenolic compounds from PNP showed selective encapsulation efficiency according to the polarity of compounds. All PNP showed antimicrobial activity against Staphylococcus aureus with a minimum inhibitory concentration ranging from 156 to 310 μg mL−1. The IC50 (the concentration responsible for reduction of cellular viability by half) for epithelial cells of bovine mammary gland (MAC-T, mammary alveolar cell-T) varied from 122.2 to 268.4 μg mL−1. Results showed that PNP represent a promising nanocarrier for high concentrations of propolis extract in a stable aqueous medium, while, at the same time, presenting antimicrobial activity accompanied by moderate cytotoxicity to the MAC-T cells.


2013 ◽  
Vol 684 ◽  
pp. 57-62 ◽  
Author(s):  
Zhi Hua Xing

Folic acid-chitosan (FA-CTS) and 10-hydroxycamptothecin (HCPT)-loaded folate-conjugated chitosan (FA-CTS/HCPT) microspheres were prepared by the ionic crosslinking method.The morphological characteristics of microspheres were examined using a scanning electron microscope (SEM). The average particle size and size distribution were determined by dynamic light scattering. The drug encapsulation efficiency (EE) , loading capacity (LC)and release characteristics in vitro were determined using ultraviolet spectrophotometer.The results shown that the microspheres are uniform spherical and regular with a size between 19.79 and81.40μm.Optimized preparation parameters lead to the successful preparation of hydroxycamptothecin-loaded folate-conjugated chitosan microspheres characterized with encapsulation efficiency and loading capacity up to (86.8±0.1)% and 20.6±0.3 % respectively. More then 90% of 10-hydroxycamptothecin was released from microspheres in 4 h at artificial gastric juice, 8h at artificial small intestinal fluid with a good delayed release effect.


Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.


2020 ◽  
Vol 189 ◽  
pp. 02010
Author(s):  
Zheng Xiaoyan ◽  
Zheng Lili ◽  
Sun Yaxin ◽  
Yang Yang ◽  
Ai Binling ◽  
...  

The soy protein isolate (SPI) was combined with tea saponin as an emulsifier to prepare camellia oil nanoemulsion, and the stability of camellia oil nanoemulsion was compared with that of soybean protein isolate or tea saponin as emulsifier. The effects of different pH, ionic strength, heating temperature and storage time on the average particle size, ξ-potential and microstructure of camellia oil nanoemulsion prepared by three emulsifiers were studied. The results showed that the nanoemulsions prepared by combining natural emulsifiers (SPI-TS) in the pH range of 5-9 were stable and remained stable in the range of 0-300mm NaCl concentration, but had poor tolerance to high salt environment. After heating at different temperatures (30 °C-90 °C) for 30min, the average particle size, ξ-potential and microstructure of the three emulsions did not change significantly, showing good heating stability. At different storage temperatures (4, 25, 50°C) SPI-TS and TS emulsion could exist stably about four weeks, and had good storage stability. In addition, we performed in vitro simulated gastrointestinal digestion studies on the digestive properties of camellia oil nanoemulsions. The results showed that the particle size, the ξ-potential of the nanoemulsion changes depend on the type of emulsifier during digestion. The release rate of free fat acids (FFAs) of nanoemulsions after gastrointestinal digestion were all higher than that of the control group. The results showed that the nanoemulsion delivery system could effectively improve the digestion of camellia oil, It was important to improve the bioavailability of camellia oil.


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