Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy

The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology. The obtained SLMs had main particle sizes ranging from 250 to 355 µm, suitable for oral administration. GSH was efficiently loaded into the SLMs at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, DSC and HSM analysis. Moreover, in vitro release studies using biorelevant media showed that Dynasan 114-based SLMs could efficiently release GSH in various intestinal fluids, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay demonstrated the good radical scavenging activity of this formulation. Dynasan 114-based SLMs exhibited an excellent biocompatibility on intestinal HT-29 cells at concentrations up to 2000 μg/mL. SLMs containing GSH alone or together with another antioxidant agent (catalase) were effective in reducing intracellular reactive oxygen species (ROS) levels. Overall, this study indicated that spray congealed SLMs are a promising oral drug delivery system for the encapsulation of one or more biological antioxidant agents for local intestinal treatment.

Download Full-text

Spray congealed solid lipid microparticles as a sustained release delivery system for Gonadorelin [6-D-Phe]: Production, optimization and in vitro release behavior

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2020.06.017 ◽

2020 ◽

Vol 154 ◽

pp. 18-32

Author(s):

Kerstin Traub-Hoffmann ◽

Katrin Gegenfurtner ◽

Kay-Uwe Kraft ◽

Wolfgang Friess

Keyword(s):

Sustained Release ◽

Delivery System ◽

In Vitro Release ◽

Production Optimization ◽

Release Behavior ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles ◽

Vitro Release

Download Full-text

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.1.3 ◽

2017 ◽

Vol 10 (1) ◽

pp. 3582-3593

Author(s):

Chukwuebuka Umeyor ◽

Uchechukwu Nnadozie ◽

Anthony Attama

Keyword(s):

Oral Delivery ◽

In Vitro Release ◽

Carrier System ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Release Study ◽

Lipid Microparticles ◽

Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Download Full-text

Efficacy of a new delivery system based on solid lipid microparticles for the oral administration of the non-conventional antioxidant IAC on a diabetes mouse model

Journal of Endocrinological Investigation ◽

10.1007/s40618-018-0858-4 ◽

2018 ◽

Vol 41 (10) ◽

pp. 1227-1236

Author(s):

D. Canistro ◽

F. Vivarelli ◽

S. Cirillo ◽

A. Soleti ◽

B. Albertini ◽

...

Keyword(s):

Mouse Model ◽

Oral Administration ◽

Delivery System ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles ◽

Diabetes Mouse

Download Full-text

Preparation and Evaluation of a Novel Oral Microemulsion Drug Delivery System for Enhancing the Bioavailability of Diltiazem

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v70i02.019 ◽

2021 ◽

Vol 70 (2) ◽

Author(s):

Ranajit Nath ◽

Ratul Bhowmik ◽

Rajarshi Chakraborty ◽

Sourav Datta ◽

Apala Chakraborty

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Drug Delivery ◽

In Vitro Release ◽

Immediate Release ◽

Oral Drug ◽

Accelerated Stability ◽

Oral Drug Delivery System

Diltiazem, a calcium ion cellular influx inhibitor is known for its limited and variable bioavailability. This study is intended to explore the benefits of microemulsion formulation as an oral drug delivery system for immediate release to improve the bioavailability and efficacy of Diltiazem. Methods: Oil in water microemulsion was prepared using the simple water titration method. The optimized formulation was evaluated for physicochemical parameters like viscosity, pH, conductivity, and accelerated stability studies. In vitro release, diltiazem microemulsion was investigated.

Download Full-text

Physicochemical Characterization of Artemether-Entrapped Solid Lipid Microparticles Prepared from Templated- Compritol and Capra hircus (Goat Fat) Homolipid

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v20i1.54034 ◽

2021 ◽

Vol 20 (1) ◽

pp. 67-80

Author(s):

Petra Obioma Nnamani ◽

Franklin Chimaobi Kenechukwu ◽

Chinekwu Sheridan Nwagwu ◽

Onyinye Okoye ◽

Anthony Amaechi Attama

Keyword(s):

Physicochemical Properties ◽

In Vitro Release ◽

Physicochemical Characterization ◽

Capra Hircus ◽

Simulated Gastric Fluid ◽

Scanning Calorimetry ◽

Simulated Intestinal Fluid ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

The purpose of this study was to formulate and evaluate the physicochemical properties of artemetherloaded solid lipid microparticles (SLM) prepared from templated-compritol 888®ATO and Capra hircus (goat fat) homolipid. Various ratios of compritol 888®ATO, goat fat and Phospholipon® 90G were used to prepare the templated lipid matrices and characterized by differential scanning calorimetry (DSC). Plain and artemether-loaded SLM (0, 1.0, 3.0 and 5.0% drug) were prepared by melt-homogenization. The SLM were characterized regarding the compatibility by DSC, morphology and particle size by polarized light microscopy (PLM), encapsulation efficiency (EE%), in vitro release in simulated gastric fluid (SGF, pH 1.2), simulated intestinal fluid (SIF, pH 7.2) and alcoholic buffer (pH 3.6), and time-resolved pH-dependent stability. Stable, smooth and mostly spherical SLM with particle sizes in the range 18.77-43.79 μm and EE% ranging from 62.22% to 99.05% were obtained. DSC results showed the compatibility of drug and the formulation excipients as well as the stability of artemether in the developed SLM. Results showed significantly (p<0.05) higher drug release (88.25%) in alcoholic buffer than in SIF and SGF. By implication, incorporation of alcohol in the formulation would be a practical approach to improve artemether bioavailability from the SLM. This study has shown that the physicochemical properties of artemether were improved by SLM based on templated-compritol 888®ATO and goat fat. Dhaka Univ. J. Pharm. Sci. 20(1): 67-80, 2021 (June)

Download Full-text

SOLID LIPID NANOPARTICLES: A PROMISING APPROACH FOR COMBINATIONAL DRUG THERAPY IN CANCER

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i5.27894 ◽

2018 ◽

Vol 10 (5) ◽

pp. 17 ◽

Cited By ~ 1

Author(s):

Rita R. Lala ◽

Amol S. Shinde ◽

Nikita Y. Nandvikar

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Solid Lipid Nanoparticles ◽

Oral Drug Delivery ◽

Lipid Nanoparticles ◽

Chemotherapeutic Agents ◽

Oral Drug ◽

Combination Drug ◽

Solid Lipid

Combination therapy for cancer treatment is accepted worldwide due to the generation of synergistic anticancer effects; restrain in multidrug resistance (MDR) or tumor resistance by different mechanisms of action and minimization of dose-dependent toxicity. Recently developed Solid lipid nanoparticles (SLNs) are matrix composed of lipid which is solid at both room and body temperature and hence it is as an alternative to other nanocarrier systems. SLNs after oral administration get absorbed by lymphatic pathway due to stimulation of chylomicron formation. Thus, it avoids all consequences related to an oral drug delivery system and improves oral bioavailability. SLNs based combination drug delivery to tumor tissues reduces the problems associated with chemotherapy. The targeted and sustained delivery of chemotherapeutic agents reduces the dose by achieving high concentrations at the target site, without altering the normal tissues. In this article, we have reviewed and focused on SLNs as a drug delivery system; ingredients used in formulating SLNs and developed two or more drugs in a single formulation of SLNs as drug delivery. This article also focuses on the fact that SLNs as a combination drug delivery provides an attractive approach in future prevention and beneficial for the treatment of cancer by increasing its therapeutic efficacy.

Download Full-text