scholarly journals Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 544
Author(s):  
Miao Wang ◽  
Sung-Kyun You ◽  
Hong-Ki Lee ◽  
Min-Gu Han ◽  
Hyeon-Min Lee ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Anticancer Agents ◽  
Lipid Membrane ◽  
Ex Vivo ◽  
System Optimization ◽  
Raw Material ◽  
Phospholipid Complex ◽  
Low Solubility

Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

Researches on Preparation of Photosan Loaded Magnetic Silica Anoparticles and their Anti-Tumor Effects in Photodynamic Therapy

2012 ◽  
Vol 622-623 ◽  
pp. 821-826
Author(s):  
Yu Wen ◽  
Xiao Feng Deng ◽  
Liang Liang Liu ◽  
Shu Yun Shi ◽  
Li Xiong
Keyword(s):  
Drug Delivery ◽  
Photodynamic Therapy ◽  
Drug Delivery System ◽  
Delivery System ◽  
Sol Gel ◽  
Haematoporphyrin Derivative ◽  
X Ray Diffraction ◽  
Transmission Electron ◽  
Good Biocompatibility ◽  
Low Solubility

Photodynamic therapy (PDT) is an effective, noninvasive and nontoxic therapeutics for cancer and some other diseases. It is becoming a alternative of traditional therapeutics for cancers. But the efficacy of PDT was restricted by insufficient selectivity and low solubility. In this study, novel multifunctional silica-based magnetic nanoparticles were prepared as targeting drug delivery system to achieve higher specificity and better solubility. Haematoporphyrin derivative (photosan) was used as photosensitizer. Magnetite nanoparticles (Fe3O4) and photosan were incorporated in silica nanoparticles by microemulsion and sol-gel methods. The prepared nanoparticles were characterized by X-ray diffraction, and transmission electron microscopy. The nanoparticles possessed good biocompatibility and could cause remarkable photodynamic anti-tumor effects. These suggested that photosan-Fe3O4 nanoparticles had great potential as effective drug delivery system in targeting photodynamic therapy.

REVIEW ON GASTRORETENTIVE DRUG DELIVERY SYSTEM

2020 ◽  
pp. 38-45
Author(s):  
MANDAR J BHANDWALKAR ◽  
PRASAD S DUBAL ◽  
AKASH K.TUPE ◽  
SUPRIYA N MANDRUPKAR
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Low Solubility

In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

scholarly journals RECENT NANOCOCHLEATE DRUG DELIVERY SYSTEM FOR CANCER TREATMENT: A REVIEW

2019 ◽  
pp. 28-32
Author(s):  
SUJIT NAYEK ◽  
ABHIRAMI VENKATACHALAM ◽  
SANGEETA CHOUDHURY
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Divalent Cation ◽  
Technology Use ◽  
Oral Bioavailability ◽  
Anticancer Agent ◽  
Low Permeability ◽  
Delivery Mechanism ◽  
Low Solubility

Nanocochleates are at the forefront of the fast-growing nanotechnology sector in the delivery of drugs for cancer. This nanotechnology is the use of the cationic and anionic encapsulated drug that has poor oral bioavailability. Nanocochleate is a lipid-based drug delivery in the liposomal vesicles that is converted by calcium divalent cation into nanocochleate. Nanocochleates technology use encapsulations of the anticancer agent, which have low solubility, oral bioavailability and low permeability. This paper shows and provides an overview of the benefits of nanocochleates, drug delivery mechanism, choice of prevalent components (Phospholipids and Cations), various ways of producing nanocochleates and nanocochleate stability. Nanocochleates have far fewer constraints than other traditional carriers. To characterize nanocochleates, the suitable analytical methods are required. Therefore, in the therapy of cancer, nanocochleate becomes commonly applied and more prospective drug delivery system.

Electro-kinetically assisted liposomal drug delivery system for characterization of ex-vivo cell-drug interactions

2014 ◽  
Vol 1688 ◽  
Author(s):  
Rajeshwari Taruvai Kalyana Kumar ◽  
Andi Wangzhou ◽  
David Kinnamon ◽  
Shalini Prasad
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Target Location ◽  
Ex Vivo ◽  
Electrical Signal ◽  
Performance Comparison ◽  
Target Cells ◽  
Label Free ◽  
Repulsive Forces

ABSTRACTThis work presents a strategy to perform ex-vivo cell-drug interaction studies through electro-kinetically assisted drug delivery system. Here, we present a novel technique to electro-kinetically control the vesicles carrying drug to deliver to pre-determined locations. In order to achieve efficient targeted drug delivery, effect of electrokinetic attractive and repulsive forces on liposomes and target cells were studied and presented. The device consists of a simple bifurcated microfluidic chamber and microelectrodes that assist in carrying the liposomes to the target location. To test the prototype, fully grown human embryonic kidney cell lines (HEK 293) and trypsin as test drug was used. External electrical signal with voltages less than of 5 V peak-to-peak (Vpp) for cells and 10 Vpp for liposomes were applied over a spectrum of frequencies to study the effect of electrokinetic forces. Through this label-free method, we were able to study loading and unloading efficiency of the drug without altering the natural properties of the liposomes and target cells. In this study, characterization and performance comparison studies for two different types of materials (HEK cells and liposomes) were performed. We were able to achieve an overall efficiency of approximately 85%. Various electrical parameters such as applied voltage, frequency and conductivity were manipulated to study the drug-cell interaction. This electrokinetic based method will be highly applicable in understanding the effect on drugs on cell populations ex vivo.

scholarly journals Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier

2012 ◽  
Vol 1 (12) ◽  
pp. 414-419 ◽  
Author(s):  
Durgacharan Arun Bhagwat ◽  
John Intru D’Souza
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Water Soluble ◽  
Solid Carrier ◽  
Drug Content ◽  
Permeability Study ◽  
Poorly Water Soluble

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419

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