Determination Of Entrapment Efficiency Research Articles

Liposomes with Caffeic Acid: Morphological and Structural Characterisation, Their Properties and Stability in Time

Medical and pharmaceutical research has shown that liposomes are very efficient in transporting drugs to targets. In this study, we prepared six liposome formulas, three in which we entrapped caffeic acid (CA), and three with only phospholipids and without CA. Determination of entrapment efficiency (EE) showed that regardless of the phospholipids used, the percentage of CA entrapment was up to 76%. The characterization of the liposomes was performed using Dynamic Light Scattering (DLS), Atomic Force Microscopy (AFM), zeta potential and polydispersity and showed that about 75–99% of the liposomes had dimensions between 40 ± 0.55–500 ± 1.45 nm. The size and zeta potential of liposomes were influenced by the type of phospholipid used to obtain them. CA release from liposomes was performed using a six-cell Franz diffusion system, and it was observed that the release of entrapped CA occurs gradually, the highest amount occurring in the first eight hours (over 80%), after which the release is much reduced. Additionally, the time stability of the obtained liposomes was analysed using univariate and multivariate statistical analysis. Therefore, liposomes offer great potential in CA entrapment.

Triggered release of paclitaxel from magnetic solid lipid nanoparticles by magnetic hyperthermia

We developed a magnetic solid lipid nanoparticles formulation of paclitaxel (PTX-loaded MSLNs) via emulsification-diffusion method. The physicochemical characterization of PTX-loaded MSLNs was performed by AFM, DLS, determination of entrapment efficiency (EE) and drug loading (DL), DSC, VSM, and physical stability. The in vitro effect of temperature and pulsed magnetic hyperthermia on drug release were studied. PTX-loaded MSLNs had a particle diameter around 250 nm with a narrow size distribution, spherical morphology, EE of 67.3 ± 1.2% and a DL of 17.1 ± 0.4 μg/mg. A decrease of the melting point of the lipid was observed following the preparation of the MSLNs. A threefold increase in the in vitro drug release rate was seen when temperature was raised from 25 to 43 °C. The lipid coating of MPs confer a temperature-dependent drug release and magnetic hyperthermia was used to trigger controlled PTX release from MSLNs.

Encapsulation challenges, the substantial issue in solid lipid nanoparticles characterization.

Solid lipid nanoparticles (SLNs), as alternative colloidal carriers, have been used for the sustained release of lipophilic drugs with poor water solubility. One of the most important parameters in the characterization of SLNs is entrapment efficiency (EE). Despite the importance of this factor in estimating the drug loading capacity, EE does not always represent the exact percentage of the entrapped drug. Several variables such as the stirring speed and duration, and concentration of surfactant, emulsifier, and drug play important roles in determining the final EE. In addition, EE is mainly affected by the type and concentration of the lipid. There are two major methods for the measurement of EE are in which the encapsulated drug in SLNs is either directly measured (direct method) or the amount of unencapsulated drug in the supernatant is measured (indirect method). Accuracy of drug analysis is the main challenge for EE calculation, and is either performed in the separated aqueous medium or the particles. In this review, we aimed to introduce the available methods for EE determination in SLNs and discuss the advantages and shortcomings of each method.

In vitro and in vivo investigation for optimization of niosomal ability for sustainment and bioavailability enhancement of diltiazem after nasal administration

Diltiazem hydrochloride (DTZ) is a calcium channel antagonist depicted by extensive first pass metabolism and low oral bioavailability. The aim of this work was to develop niosomes for potential nasal delivery of DTZ. Niosomes protect hydrophilic drugs inside their core while nasal route offers both rapid onset and evasion of first-pass metabolism. Niosomes were prepared using a combination of Span 60 or Brij-52 with cholesterol (CHOL) in different molar ratios followed by determination of entrapment efficiency, particle size and in vitro drug release. A parallel design was adopted to evaluate the pharmacokinetic performance of DTZ-loaded niosomes in male Wistar rats. Non-compartmental analysis was performed where Cmax, Tmax, t1/2, MRT, area under the release curve (AUC) and Ke were assessed. The prepared niosomes were spherical with mean particle size 0.82–1.59 μm. Span 60-cholesterol niosomes (1:1 molar ratio) showed the highest entrapment and release efficiencies. In vivo study revealed an increase in MRT, t1/2 and AUC with a decrease in Ke. In conclusion, nasal niosomal formulation of DTZ expressed suitable pharmacokinetic parameters and bioavailability through prolonged duration of action inside the body as well as low rate of elimination depicting a promising alternate to the conventional oral route.

The Study on the Entrapment Efficiency and In Vitro Release of Puerarin Submicron Emulsion

The entrapment efficiency (EE) and release in vitro are very important physicochemical characteristics of puerarin submicron emulsion (SME). In this paper, the performance of ultrafiltration (UF), ultracentrifugation (UC), and microdialysis (MD) for determining the EE of SME were evaluated, respectively. The release study in vitro of puerarin from SME was studied by using MD and pressure UF technology. The EE of SME was 86.5%, 72.8%, and 55.8% as determined by MD, UF, and UC, respectively. MD was not suitable for EE measurements of puerarin submicron oil droplet, which could only determine the total EE of submicron oil droplet and liposomes micelles, but it could be applied to determine the amount of free drug in SMEs. Although UC was the fastest and simplest to use, its results were the least reliable. UF was still the relatively accurate method for EE determination of puerarin SME. The release of puerarin SME could be evaluated by using MD and pressure UF, but MD seemed to be more suitable for the release study of puerarin emulsion. The drug release from puerarin SME at three drug concentrations was initially rapid, but reached a plateau value within 30 min. Drug release of puerarin from the SME occurred via burst release.

Determination of entrapment efficiency and drug phase distribution of submicron emulsions loaded silybin

This paper compared the performance of ultrafiltration (UF), ultracentrifugation (UC) and microdialysis (MD) for determining the entrapment efficiency (EE) of submicron emulsions (SE) loaded with a model drug, silybin (SB). Also, a novel way was created to evaluate the drug phase distribution of SE. The EE of SEI, SEII and SEIII with a range of particle sizes (109.8, 171.7 and 213.2 nm) and the drug phase distribution of SEII and SEIII were separately determined by the three methods. The EEs of SEI were 99.8%, 91.1%, 84.4% determined by MD, UF, UC, respectively, and the EEs of SEII and SEIII were 99.5%, 86.4%, 72.1% and 99.4%, 84.3%, 66.3%, separately. The accuracy of MD to determine EE of SE is much less than that of UF. Although UC is the fastest and most simple to use, its results are the least reliable. The sequence of the amount of drug in SE is as follows: O/W interface, aqueous phase and oil phase. Over 80% of SB was in the O/W interface of SEII and SEIII individually. The method created is reliable for quantifying the phase distribution of drug in submicron emulsions.