scholarly journals Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1052
Author(s):  
Reem Abou Assi ◽  
Ibrahim M. Abdulbaqi ◽  
Toh Seok Ming ◽  
Chan Siok Yee ◽  
Habibah A. Wahab ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Bacterial Infections ◽  
Drug Delivery Systems ◽  
Storage Conditions ◽  
Delivery Systems ◽  
Drug Dissolution ◽  
In Vitro Characterization ◽  
Low Solubility

Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.

scholarly journals Effects of Hydrophilic Carriers on Structural Transitions and In Vitro Properties of Solid Self-Microemulsifying Drug Delivery Systems

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 267 ◽  
Author(s):  
Tao Yi ◽  
Jifen Zhang
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Commercial Application ◽  
Simulated Gastric Fluid ◽  
Structural Transitions

Self-microemulsifying drug delivery systems (SMEDDS) offer potential for improving the oral bioavailability of poorly water-soluble drugs. However, their susceptibilities during long term storage and in vivo precipitation issues limit their successful commercial application. To overcome these limitations, SMEDDS can be solidified with solid carriers, thus producing solid self-microemulsifying drug delivery systems (S-SMEDDS). In this study, effects of various hydrophilic carriers on structural transitions and in vitro properties of S-SMEDDS were investigated in order to set up in vitro methods for screening out appropriate carriers for S-SMEDDS. Liquid SMEDDS was prepared and characterized using nimodipine as a model drug. The effects of various hydrophilic carriers on internal microstructure and solubilization of SMEDDS were investigated by conductivity measurement and in vitro dispersion test. The results showed that hydrophilic carriers including dextran 40, maltodextrin and PVP K30 seemed to delay the percolation transition of SMEDDS, allowing it to maintain a microstructure that was more conducive to drug dissolution, thus significantly increasing the solubilization of nimodipine in the self-microemulsifying system and decreasing drug precipitation when dispersed in simulated gastric fluid. S-SMEDDS of nimodipine were prepared by using spray drying with hydrophilic carriers. The effects of various hydrophilic carriers on in vitro properties of S-SMEDDS were investigated by using SEM, DSC, PXRD and in vitro dissolution. The results showed that properties of hydrophilic carriers, especially relative molecular mass of carriers, had obvious influences on surface morphologies of S-SMEDDS, reconstitution of microemulsion and physical state of nimodipine in S-SMEDDS. Considering that in vitro properties of S-SMEDDS are closely related to their pharmacokinetic properties in vivo, the simple and economical in vitro evaluation methods established in this paper can be used to screen solid carriers of S-SMEDDS well.

Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) Containing Rice Bran Oil for Enhanced Fenofibrate Oral Delivery: In Vitro Digestion, Ex Vivo Permeability, and In Vivo Bioavailability Studies

2020 ◽  
Vol 21 (6) ◽  
Author(s):  
Christina Karavasili ◽  
Ioannis I. Andreadis ◽  
Maria P. Tsantarliotou ◽  
Ioannis A. Taitzoglou ◽  
Paschalina Chatzopoulou ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Rice Bran ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Rice Bran Oil ◽  
Ex Vivo ◽  
In Vitro Digestion ◽  
Delivery Systems

scholarly journals Engineered Remolding and Application of Bacterial Membrane Vesicles

2021 ◽  
Vol 12 ◽  
Author(s):  
Li Qiao ◽  
Yifan Rao ◽  
Keting Zhu ◽  
Xiancai Rao ◽  
Renjie Zhou
Keyword(s):  
Drug Delivery ◽  
Bacterial Infections ◽  
Drug Delivery Systems ◽  
Membrane Vesicles ◽  
Delivery Systems ◽  
Bacterial Membrane ◽  
Wild Type ◽  
Bacterial Strains

Bacterial membrane vesicles (MVs) are produced by both Gram-positive and Gram-negative bacteria during growth in vitro and in vivo. MVs are nanoscale vesicular structures with diameters ranging from 20 to 400 nm. MVs incorporate bacterial lipids, proteins, and often nucleic acids, and can effectively stimulate host immune response against bacterial infections. As vaccine candidates and drug delivery systems, MVs possess high biosafety owing to the lack of self-replication ability. However, wild-type bacterial strains have poor MV yield, and MVs from the wild-type strains may be harmful due to the carriage of toxic components, such as lipopolysaccharides, hemolysins, enzymes, etc. In this review, we summarize the genetic modification of vesicle-producing bacteria to reduce MV toxicity, enhance vesicle immunogenicity, and increase vesicle production. The engineered MVs exhibit broad applications in vaccine designs, vaccine delivery vesicles, and drug delivery systems.

Lipid Nanocarriers for Oral Delivery of Serenoa repens CO2 Extract: A Study of Microemulsion and Self-Microemulsifying Drug Delivery Systems

Planta Medica ◽  
2018 ◽  
Vol 84 (09/10) ◽  
pp. 736-742 ◽  
Author(s):  
Clizia Guccione ◽  
Maria Bergonzi ◽  
Khaled Awada ◽  
Vieri Piazzini ◽  
Anna Bilia
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Absorption ◽  
Delivery Systems ◽  
Array Detector ◽  
Serenoa Repens ◽  
Lipid Nanocarriers

AbstractThe aim of this study was the development and characterization of lipid nanocarriers using food grade components for oral delivery of Serenoa repens CO2 extract, namely microemulsions (MEs) and self-microemulsifying drug delivery systems (SMEDDSs) to improve the oral absorption. A commercial blend (CB) containing 320 of S. repens CO2 extract plus the aqueous soluble extracts of nettle root and pineapple stem was formulated in two MEs and two SMEDDSs. The optimized ME loaded with the CB (CBM2) had a very low content of water (only 17.3%). The drug delivery systems were characterized by dynamic light scattering, transmission electron microscopy, and high-performance liquid chromatography (HPLC) with a diode-array detector analyses in order to evaluate the size, the homogeneity, the morphology, and the encapsulation efficiency. β-carotene was selected as marker for the quantitative HPLC analysis. Additionally, physical and chemical stabilities were acceptable during 3 wk at 4 °C. Stability of these nanocarriers in simulated stomach and intestinal conditions was proved. Finally, the improvement of oral absorption of S. repens was studied in vitro using parallel artificial membrane permeability assay. An enhancement of oral permeation was found in both CBM2 and CBS2 nanoformulations comparing with the CB and S. repens CO2 extract. The best performance was obtained by the CBM2 nanoformulation (~ 17%) predicting a 30 – 70% passive oral human absorption in vivo.

scholarly journals Formulation and characterisation of self-microemulsifying drug delivery systems based on biocompatible nonionic surfactants

2014 ◽  
Vol 68 (5) ◽  
pp. 565-573 ◽  
Author(s):  
Ljiljana Djekic ◽  
Marija Primorac
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Aqueous Media ◽  
Delivery Systems ◽  
Medium Chain Triglycerides ◽  
Medium Chain

Development of self-dispersing drug delivery systems (SMEDDS) is a modern strategy for oral delivery improvement of poorly soluble drugs. Self-microemulsifying drug delivery systems (SMEDDS) are isotropic mixtures of oils and hydrophilic surfactants, which form oil-in-water (o/w) microemulsions by dilution in aqueous media (e.g., gastrointestinal fluids). Formulation of SMEDDS carriers requires consideration of a large number of formulation parameters and their influences on process of self-microemulsifying and releasing of drug. The aim of this work was formulation and characterisation of SMEDDS for oral administration of ibuprofen. In the experimental work, two series of potential SMEDDS were prepared (M1-M10), using surfactant (Labrasol?, Gattefosse), cosurfactant (PEG-40 hydrogenated castor (Cremophor? RH40), and oil (medium chain triglycerides (Crodamol? GTCC) and olive oil (Cropur? Olive)), at surfactant-to-cosurfactant mass ratios (Km) 9:1, 7:3, 5:5, 3:7, and 1:9, and 10 % or 20 % of the oil phase. Ibuprofen was dissolved in formulations in concentration of 10 %. Characterisation of the investigated formulations included evaluation of physical stability, self-microemulsification ability in 0,1M HCl (pH 1.2) and phosphate buffer pH 7.2 (USP) and in vitro drug release. Formation of o/w microemulsions with the average droplet size (Z-ave) up to 100 nm, was observed in dispersions of formulations prepared with 10% w/w of medium chain triglycerides, within the entire investigated range of the Km values (M1-M5). These formulations were selected as SMEDDS. Results of characterisation pointed out the importance of the type and concentration of the oil as well as the Km value for the self-microemulsying ability as well as drug release kinetics from the investigated SMEDDS. Ibuprofen relase was in accordance with the request of USP 30-NF 25 (at least 80 %, after 60 min) from the formulations M1 (Km 9:1) and M5 (Km 1:9). Furthermore, ibuprofen release was completed after 10 minutes from formulation M1, while the release from the carrier M5 (~30 %) as well as from the commercial tablets Brufen? (~55%) and soft capsules Rapidol? (~65 %), examined under the same conditions, was significantly slower. The present study revealed that the formulation M1 represents a potential SMEDDS which efficiently solubilises ibuprofen in acidic media, with potential to minimise the side effects, while on introduction into alkaline intestinal environment, the drug may rapidly release from the carrier and undergo apsorption.

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