scholarly journals Integration of PEG 400 into a self-nanoemulsifying drug delivery system improves drug loading capacity and nasal mucosa permeability and prolongs the survival of rats with malignant brain tumors

2019 ◽  
Vol Volume 14 ◽  
pp. 3601-3613 ◽  
Author(s):  
Yu-Shuan Chen ◽  
Yu-Han Chiu ◽  
Yuan-Sheng Li ◽  
En-Yi Lin ◽  
Dean-Kuo Hsieh ◽  
...  
2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Jinglei Du ◽  
Qiang Li ◽  
Lin Chen ◽  
Shicai Wang ◽  
Li Zhang ◽  
...  

A dual-targeting drug delivery system (DTDDS) with magnetic targeting and active targeting was obtained to improve the targeting and drug-loading capacity of magnetic drug nanocarriers. An ultraviolet-visible spectrophotometer and flow cytometry were used to investigate the drug-loading and release capacity, cytotoxicity, and inhibition of tumor cell proliferation, separately. Results show that DTDDS has obvious magnetic characteristics, on which the modification amount of folic acid is 64.82 mg g-1. Doxorubicin was taken as a template drug to evaluate its drug-loading capacity, which was as high as 577.12 mg g-1. Good biocompatibility and low cytotoxicity of DTDDS were further confirmed. Moreover, DTDDS can target the folate receptor on the surface of HeLa cells and deliver doxorubicin into HeLa cells, thereby increasing the proliferation inhibition for cancer cells. Therefore, this new dual-targeting drug delivery system shows potential in significantly reducing the toxic side effects of chemotherapy and improving chemotherapy efficiency.


2017 ◽  
Vol 14 (2) ◽  
pp. 99-109
Author(s):  
Ilham Kuncahyo ◽  
Pudiastuti RSP

Kurkumin terbukti memiliki aktivitas sebagai anti-tumor, anti-inflamasi, anti-virus, anti-oksidasi dan anti HIV. Penggunaan kurkumin dalam proses pengobatan jangka panjang memberikan toksisitas yang rendah sehingga secara klinis akan sangat menguntungkan untuk dikembangkan. Kandungan aktif kurkumin yang berasal dari ekstrak tanaman curcuma longa ini mempunyai bioavaiblitas yang sangat rendah. Hal ini berkaitan karena kelarutan kurkumin yang jelek dalam air (11 ng/ml, pH 5,0) sehingga sedikit diserap di saluran pencernaan. Permasalahan ini dapat diatasi dengan membuat sediaan kurkumin dalam bentuk Self Mikroemulsi Drug Delivery System (SMEDDS) Penelitian awal dilakukan skrining terhadap kelarutan kurkumin dengan pembawa berbagai jenis minyak, surfaktan dan kosurfaktan. Hasil skrining dilanjutkan dengan pemilihan formula optimum SMEDDS kurkumin dengan menggunakan metode Simpelx Lattice Design (SLD). Tiga variabel akan memberikan 14 formula SMEDDS kurkumin yang masing-masing formula dilakukan pengujian terhadap karakteristiknya sebagai titik kritis meliputi : % transmitan, waktu emulsifikasi dan drug loading. Hasil masing-masing pengujian dianalisis datanya dengan Design Exspert versi 7 dan dilanjutnya validasi formula optimum dengan uji T dengan taraf kepercayaan 95%. Hasil penelitian menunjukkan bahwa skrining awal terhadap kurkumin didapatkan kelarutan yang terbesar pada jenis minyak zaitun, surfaktan Tween 80 dan kosurfaktan PEG 400. Ketiga jenis bahan ini dilakukan optimasi dengan SLD memberikan formula optimum komposisi SMEDDS kurkumin dengan komposisi 0,026 minyak zaitun ; 0,0913 Tween 80 dan 0,061 PEG 400.


2020 ◽  
Vol 1 (2) ◽  
pp. 27-34
Author(s):  
Septiana Indratmoko ◽  
Asep Nurrahman ◽  
Axl Aprizal Herawan

Kandungan flavonoid dan tanin pada daun kersen dapat  menghambat pertumbuhan bakteri Staphylococcus aureus. Penelitian ini bertujuan untuk mengetahui pengaruh formulasi nanoemulsi daun kersen (Mutingia calabura.L) terhadap karakteristik nanoemulsi menggunakan teknik Self Nano Emulsifying Drug Delivery System (SNEDDS) dan  pengaruhnya sebagai antibakteri Staphylococcus aureus. Ekstrak etanol daun kersen diformulasi dengan surfaktan, kosurfaktan dan minyak terpilih. Kemudian nanoemulsi ekstrak daun kersen diuji ukuran partikel, potensial zeta, drug loading dan stabilitas nanoemulsi. Nanoemulsi ekstrak etanol daun kersen dapat dihasilkan dengan formula Tween 80, PEG 400 dan VCO perbandingan 6:1:1. Ukuran partikel nanoemulsi 12,4 nm, potensial zeta 30,8 mV, drug loading yaitu 125 mg/ml dan stabil. Nanoemulsi ekstrak daun kersen dapat memberikan aktivitas antibakteri lebih baik daripada ekstrak daun kersen.


Author(s):  
Prabhat Kumar Sahoo ◽  
Neha S.L ◽  
Arzoo Pannu

Lipids are used as vehicles for the preparation of various formulations prescribed for administrations, including emulsions, ointments, suspension, tablets, and suppositories. The first parental nano-emulsion was discovered from the 1950s when it was added to the intravenous administration of lipid and lipid-soluble substances. Lipid-based drug delivery systems are important nowadays. Solid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) are very proficient due to the ease of production process, scale-up capability, bio-compatibility, the biodegradability of formulation components and other specific features of the proposed route. The administration or nature of the materials must be loaded into these delivery systems. The main objectives of this review are to discuss an overview of second-generation nanoparticles, their limitations, structures, and route of administration, with emphasis on the effectiveness of such formulations. NLC is the second generation of lipid nanoparticles having a structure like nanoemulsion. The first generation of nanoparticles was SLN. The difference between both of them is at its core. Both of them are a colloidal carrier in submicron size in the range of 40-1000 nm. NLC is the most promising novel drug delivery system over the SLN due to solving the problem of drug loading and drug crystallinity. Solid and liquid lipids combination in NLC formation, improve its quality as compare to SLN. NLC has three types of structures: random, amorphous, and multiple. The random structure containing solid-liquid lipids and consisting crystal and the liquid lipid irregular in shape; thereby enhance the ability of the lipid layer to pass through the membrane. The second is the amorphous structure. It is less crystalline in nature and can prevent the leakage of the loaded drug. The third type is multiple structures, which have higher liquid lipid concentrations than other types. The excipients used to form the NLC are bio-compatible, biodegradable and non-irritating, most of which can be detected using GRAS. NLC is a promising delivery system to deliver the drug through pulmonary, ocular, CNS, and oral route of administration. Various methods of preparation and composition of NLC influence its stability Parameters. In recent years at the educational level, the potential of NLC as a delivery mechanism targeting various organs has been investigated in detail.


Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla

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.  


Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.


2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.


2020 ◽  
Vol 35 (1) ◽  
pp. 15-27 ◽  
Author(s):  
Taicheng Lu ◽  
Zhenzhen Nong ◽  
Liying Wei ◽  
Mei Wei ◽  
Guo Li ◽  
...  

In this study, a transferrin/folic acid double-targeting graphene oxide drug delivery system loaded with doxorubicin was designed. Graphene oxide was prepared by ultrasound improved Hummers method and was modified with Pluronic F68, folic acid, and transferrin to decrease its toxicity and to allow dual-targeting. The results show that the double target drug delivery system (TFGP*DOX) has good and controllable drug delivery performance with no toxicity. Moreover, TFGP*DOX has a better inhibitory effect on SMMC-7721 cells than does a single target drug delivery system (FGP*DOX). The results of drug release analysis and cell inhibition studies showed that TFGP*DOX has a good sustained release function that can reduce the drug release rate in blood circulation over time and improve the local drug concentration in or near a targeted tumor. Therefore, the drug loading system (TFGP*DOX) has potential application value in the treatment of hepatocellular carcinoma.


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