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

Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata

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2014
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Đekić, Ljiljana
Primorac, Marija
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Abstract
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 characterization 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 (PEG­40 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%. Characterization of the investigated formulations included evaluation of physical stability, self-microemulsification ability in 0.1 M 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 mass% of medium chain triglycerides, within the entire investigated range of the Km values (M1-M5). These formulations were selected as SMEDDS. Results of characterization pointed out the importance of the type and concentration of the oil as well as the Km value for the self-microemulsing ability, as well as drug release kinetics from the investigated SMEDDS. Ibuprofen release 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, the ibuprofen release was completed after 10 min 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 dissolves ibuprofen in acidic media, with potential to minimize the side effects, while on introduction into alkaline intestinal environment, the drug may rapidly release from the carrier and undergo absorption.

Razvoj samo-mikroemulgujućih nosača je značajna savremena strategija za unapređenje peroralne primene teško rastvorljivih aktivnih supstanci. Cilj rada bio je formulacija i karakterizacija samo-mikroemulgujućih nosača na bazi smeše biokompatibilnih nejonskih surfaktanata (PEG-8 kaprilno/kaprinski gliceridi (Labrasol®) i PEG-40 hidrogenizovano ricinusovo ulje (Cremophor® RH40)) za peroralnu primenu ibuprofena i in vitro karakterizacija njihove fizičke stabilnosti i veličine kapi nakon dispergovanja u vodenim medijumima različite pH vrednosti i in vitro profila oslobađanja lekovite supstance iz nosača. Rezultati karakterizacije ukazali su na značaj vrste i koncentracije ulja i masenog odnosa upotrebljenih surfaktanata za sposobnost samo-mikroemulgovanja, kapacitet za solubilizaciju ibuprofena i njegovu brzinu oslobađanja iz nosača.
Keywords:
Self-microemulsifying drug delivery systems (SMEDDS) / Microemulsions / Labrasol® / Cremophor® RH40 / Ibuprofen / samo-mikroemulgujući nosači lekovitih supstanci / mikroemulzije / Labrasol® / Cremophor® RH40 / ibuprofen
Source:
Hemijska industrija, 2014, 68, 5, 565-573
Publisher:
  • Savez hemijskih inženjera, Beograd
Projects:
  • Novel encapsulation and enzyme technologies for designing of new biocatalysts and biologically active compounds targeting enhancement of food quality, safety and competitiveness (RS-46010)
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)

DOI: 10.2298/HEMIND130825083D

ISSN: 0367-598X

WoS: 000346394000006

Scopus: 2-s2.0-84922594258
[ Google Scholar ]
3
2
URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/2286
Collections
  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy
TY  - JOUR
AU  - Đekić, Ljiljana
AU  - Primorac, Marija
PY  - 2014
UR  - http://farfar.pharmacy.bg.ac.rs/handle/123456789/2286
AB  - 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 characterization 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 (PEG­40 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%. Characterization of the investigated formulations included evaluation of physical stability, self-microemulsification ability in 0.1 M 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 mass% of medium chain triglycerides, within the entire investigated range of the Km values (M1-M5). These formulations were selected as SMEDDS. Results of characterization pointed out the importance of the type and concentration of the oil as well as the Km value for the self-microemulsing ability, as well as drug release kinetics from the investigated SMEDDS. Ibuprofen release 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, the ibuprofen release was completed after 10 min 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 dissolves ibuprofen in acidic media, with potential to minimize the side effects, while on introduction into alkaline intestinal environment, the drug may rapidly release from the carrier and undergo absorption.
AB  - Razvoj samo-mikroemulgujućih nosača je značajna savremena strategija za unapređenje peroralne primene teško rastvorljivih aktivnih supstanci. Cilj rada bio je formulacija i karakterizacija samo-mikroemulgujućih nosača na bazi smeše biokompatibilnih nejonskih surfaktanata (PEG-8 kaprilno/kaprinski gliceridi (Labrasol®) i PEG-40 hidrogenizovano ricinusovo ulje (Cremophor® RH40)) za peroralnu primenu ibuprofena i in vitro karakterizacija njihove fizičke stabilnosti i veličine kapi nakon dispergovanja u vodenim medijumima različite pH vrednosti i in vitro profila oslobađanja lekovite supstance iz nosača. Rezultati karakterizacije ukazali su na značaj vrste i koncentracije ulja i masenog odnosa upotrebljenih surfaktanata za sposobnost samo-mikroemulgovanja, kapacitet za solubilizaciju ibuprofena i njegovu brzinu oslobađanja iz nosača.
PB  - Savez hemijskih inženjera, Beograd
T2  - Hemijska industrija
T1  - Formulation and characterisation of self-microemulsifying drug delivery systems based on biocompatible nonionic surfactants
T1  - Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata
VL  - 68
IS  - 5
SP  - 565
EP  - 573
DO  - 10.2298/HEMIND130825083D
ER  - 
@article{
author = "Đekić, Ljiljana and Primorac, Marija",
year = "2014",
url = "http://farfar.pharmacy.bg.ac.rs/handle/123456789/2286",
abstract = "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 characterization 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 (PEG­40 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%. Characterization of the investigated formulations included evaluation of physical stability, self-microemulsification ability in 0.1 M 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 mass% of medium chain triglycerides, within the entire investigated range of the Km values (M1-M5). These formulations were selected as SMEDDS. Results of characterization pointed out the importance of the type and concentration of the oil as well as the Km value for the self-microemulsing ability, as well as drug release kinetics from the investigated SMEDDS. Ibuprofen release 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, the ibuprofen release was completed after 10 min 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 dissolves ibuprofen in acidic media, with potential to minimize the side effects, while on introduction into alkaline intestinal environment, the drug may rapidly release from the carrier and undergo absorption., Razvoj samo-mikroemulgujućih nosača je značajna savremena strategija za unapređenje peroralne primene teško rastvorljivih aktivnih supstanci. Cilj rada bio je formulacija i karakterizacija samo-mikroemulgujućih nosača na bazi smeše biokompatibilnih nejonskih surfaktanata (PEG-8 kaprilno/kaprinski gliceridi (Labrasol®) i PEG-40 hidrogenizovano ricinusovo ulje (Cremophor® RH40)) za peroralnu primenu ibuprofena i in vitro karakterizacija njihove fizičke stabilnosti i veličine kapi nakon dispergovanja u vodenim medijumima različite pH vrednosti i in vitro profila oslobađanja lekovite supstance iz nosača. Rezultati karakterizacije ukazali su na značaj vrste i koncentracije ulja i masenog odnosa upotrebljenih surfaktanata za sposobnost samo-mikroemulgovanja, kapacitet za solubilizaciju ibuprofena i njegovu brzinu oslobađanja iz nosača.",
publisher = "Savez hemijskih inženjera, Beograd",
journal = "Hemijska industrija",
title = "Formulation and characterisation of self-microemulsifying drug delivery systems based on biocompatible nonionic surfactants, Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata",
volume = "68",
number = "5",
pages = "565-573",
doi = "10.2298/HEMIND130825083D"
}
Đekić L, Primorac M. Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata. Hemijska industrija. 2014;68(5):565-573
Đekić, L.,& Primorac, M. (2014). Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata.
Hemijska industrijaSavez hemijskih inženjera, Beograd., 68(5), 565-573.
https://doi.org/10.2298/HEMIND130825083D
Đekić Ljiljana, Primorac Marija, "Formulacija i karakterizacija samo-mikroemulgujućih nosača lekovitih supstanci na bazi biokompatibilnih nejonskih surfaktanata" 68, no. 5 (2014):565-573,
https://doi.org/10.2298/HEMIND130825083D .

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