scholarly journals Chitosan-based nanoparticles for improved anticancer efficacy and bioavailability of mifepristone

2016 ◽  
Vol 7 ◽  
pp. 1861-1870 ◽  
Author(s):  
Huijuan Zhang ◽  
Fuqiang Wu ◽  
Yazhen Li ◽  
Xiping Yang ◽  
Jiamei Huang ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Delivery System ◽  
Water Solubility ◽  
Release Kinetics ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Male Rats ◽  
Spherical Particles ◽  
Pharmacokinetic Studies

In addition to its well-known abortifacient effect, mifepristone (MIF) has been used as an anticancer drug for various cancers in many studies with an in-depth understanding of the mechanism of action. However, application of MIF is limited by its poor water solubility and low oral bioavailability. In this work, we developed a drug delivery system based on chitosan nanoparticles (CNs) to improve its bioavailability and anticancer activity. The MIF-loaded chitosan nanoparticles (MCNs) were prepared by convenient ionic gelation techniques between chitosan (Cs) and tripolyphosphate (TPP). The preparation conditions, including Cs concentration, TPP concentration, Cs/MIF mass ratio, and pH value of the TPP solution, were optimized to gain better encapsulation efficiency (EE) and drug loading capacity (DL). MCNs prepared with the optimum conditions resulted in spherical particles with an average size of 200 nm. FTIR and XRD spectra verified that MIF was successfully encapsulated in CNs. The EE and DL of MCNs determined by HPLC were 86.6% and 43.3%, respectively. The in vitro release kinetics demonstrated that MIF was released from CNs in a sustained-release manner. Compared with free MIF, MCNs demonstrated increased anticancer activity in several cancer cell lines. Pharmacokinetic studies in male rats that were orally administered MCNs showed a 3.2-fold increase in the area under the curve from 0 to 24 h compared with free MIF. These results demonstrated that MCNs could be developed as a potential delivery system for MIF to improve its anticancer activity and bioavailability.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

scholarly journals Development and characterization of phytosterol nanoemulsions and self-microemulsifying drug delivery systems

2019 ◽  
Author(s):  
Yuan Chuanxun ◽  
Zhang Xueru ◽  
Jin Risheng
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Drug Loading ◽  
In Vitro Release ◽  
Pharmacokinetic Analysis ◽  
Polyethylene Glycol 400 ◽  
Hydrogenated Castor Oil ◽  
Release Curve ◽  
Tween 60

AbstractThe aim of this study is to develop a self microemulsion drug delivery system for phytosterols to improve the solubility and bioavailability. The results showed that the formulation of phytosterol self-microemulsion is: lemon essential oil in oil phase, polyoxyethylene hydrogenated castor oil 40 and Tween 60 in emulsifier, polyethylene glycol 400 in co-emulsifier, Km = 7:3, Kp = 3:1, Ke = 50%. The drug loading of phytosterol self-microemulsion prepared by this method was 87.22 mg/g, encapsulation efficiency was 89.65%, particle size was 48.85nm, potential was −12.863mV. In vitro release experiment showed that the release of phytosterols in microemulsion was more than 90%, and the release curve was in accordance with the first-order kinetics equation. The pharmacokinetic analysis of PSSM synthesized by this method shows that PSSM can increase the bioavailability of PS more than three times, so it is necessary to do more in-depth research on the self-microemulsion delivery system of phytosterols.

scholarly journals DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

2021 ◽  
pp. 120-125
Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Release Kinetics ◽  
Ph Effect ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

Denatured collagen as support for a FGF-2 delivery system: physicochemical characterizations and in vitro release kinetics and bioactivity

Biomaterials ◽  
2004 ◽  
Vol 25 (17) ◽  
pp. 3761-3772 ◽  
Author(s):  
Marie-France Côté ◽  
Gaetan Laroche ◽  
Edith Gagnon ◽  
Pascale Chevallier ◽  
Charles J Doillon
Keyword(s):  
Delivery System ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Vitro Release

scholarly journals Effects of Different Drying Methods on the Characterization, Dissolution Rate and Antioxidant Activity of Ursolic Acid-Loaded Chitosan Nanoparticles

Foods ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 2470
Author(s):  
Lujie Zhao ◽  
Xu Duan ◽  
Weiwei Cao ◽  
Xing Ren ◽  
Guangyue Ren ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
Ursolic Acid ◽  
Freeze Drying ◽  
Water Solubility ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Simulated Gastric Fluid ◽  
Drying Methods ◽  
Drying Time

To improve the water solubility of ursolic acid (UA), UA-loaded chitosan nanoparticles were firstly prepared by the ionotropic gelation method and dried by freeze drying (FD), microwave freeze drying (MFD) and spray drying (SD). The characterization of UA-loaded chitosan nanoparticles was performed with particle size, drug loading (DL), scanning electron microscope (SEM), fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), dissolution studies and antioxidant activity. The results demonstrated that UA was successfully encapsulated into chitosan nanoparticles using sodium tripolyphosphate (TPP) as a cross-linker, with a 79% encapsulation efficiency. The spray-dried, UA-loaded chitosan nanoparticles had the lowest drug loading (11.8%) and the highest particle size (496.9 ± 11.20 nm). The particle size of UA-loaded chitosan nanoparticles dried by MFD and FD was lower, at 240.8 ± 12.10 nm and 184.4 ± 10.62 nm, respectively, and their antioxidant activity was higher than those nanoparticles dried by SD. Moreover, the drying time and energy consumption of UA-loaded chitosan nanoparticles dried by MFD and SD were lower than that of FD. The dissolution rates of UA-loaded chitosan nanoparticles prepared by FD and MFD were 60.6% and 57.1%, respectively, in a simulated gastric fluid, which was a greater value than SD (55.9%). Therefore, the UA-loaded chitosan nanoparticles encapsulation method, combined with MFD technology, showed a promising potential to improve the water solubility of UA.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

Quaternized Chitosan Nanoparticles in Vaccine Applications

2020 ◽  
Vol 27 (30) ◽  
pp. 4932-4944 ◽  
Author(s):  
Shuang Yu ◽  
Shengnan Hao ◽  
Beini Sun ◽  
Dongying Zhao ◽  
Xingye Yan ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Delivery System ◽  
Dilute Hydrochloric Acid ◽  
Water Solubility ◽  
Chitosan Nanoparticles ◽  
Research Direction ◽  
Acidic Solutions ◽  
Quaternized Chitosan ◽  
Inorganic Acids ◽  
Biomedical Field

Different natural and synthetic biodegradable polymers have been used in vaccine formulations as adjuvant and delivery system but have faced various limitations. Chitosan is a new delivery system with the potential to improve development of nano vaccines and drugs. However, chitosan is only soluble in acidic solutions of low concentration inorganic acids such as dilute acetic acid and dilute hydrochloric acid and in pure organic solvents, which greatly limits its application. Chemical modification of chitosan is an important way to improve its weak solubility. Quaternized chitosan not only retains the excellent properties of chitosan, but also improves its water solubility for a wider application. Recently, quaternized chitosan nanoparticles have been widely used in biomedical field. This review focuses on some quaternized chitosan nanoparticles, and points out the advantages and research direction of quaternized chitosan nanoparticles. As shown by the applications of quaternized chitosan nanoparticles as adjuvant and delivery carrier in vaccines, quaternized chitosan nanoparticles have promising potential in application for the development of nano vaccines in the future.

Formulation and Optimization of Solid-Lipid Nano-particles of the Anticancer Drug Bortezomib

2019 ◽  
Vol 12 (2) ◽  
pp. 4461-4475
Author(s):  
Taraka Sunil Kumar K ◽  
M. Mohan Varma ◽  
Ravi Prakash P
Keyword(s):  
Release Kinetics ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Cancer Drug ◽  
Solid Lipid ◽  
Zero Order Release ◽  
Presystemic Metabolism

Solid-lipid nanoparticles (SLNs) are an alternative carrier system used for loading the drug for targeting, improving the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nanometric size range so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Bortezomib is an anti-cancer drug. Due to its poor oral bioavailability, presystemic metabolism and decreased half-life, it was chosen to formulate as the SLN system with the use of a 3-factor, 3-level Box–Behnken design, by hot homogenization followed by an ultrasonication method. Trimyristin (Dynasan-114), tripalmitin (Dynasan 116) and tristearin (Dynasan-118) were used as lipids and based on the results from the initial studies tripalmitin (Dynasan116) was selected as the lipid for the further studies along with phosphatidylcholine as surfactant and Poloxamer 188 as stabilizer. The optimized formulation (F1) was obtained with minimum particle size (204 nm), maximum entrapment efficiency (70.24) and drug loading (21.24). The optimised batches were further investigated by FTIR, DSC, XRD, SEM and stability. In vitro release studies showed that maximum cumulative drug release was obtained for F1 (99.74%). The optimized formulation Bortezomib followed zero-order release kinetics with a strong correlation coefficient (R2= 0.9994). The nanoformulation prepared under optimized conditions is in concurrence with the expected results. It is concluded that the SLN formulation can be used as a potential carrier for the effective delivery of Bortezomib.

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