scholarly journals Rapid and Sensitive Analytical Method for the Determination of Insulin in Liposomes by Reversed-Phase HPLC

2020 ◽  
Vol 67 (4) ◽  
pp. 1273-1280
Author(s):  
Eliete de Souza Von Zuben ◽  
Josimar Oliveira Eloy ◽  
Victor Hugo Sousa Araujo ◽  
Maria Palmira Daflon Gremião ◽  
Marlus Chorilli

Insulin is an important anabolic hormone that regulates the metabolism of carbohydrates, lipids and proteins. In this study, a reverse-phase liquid chromatography (RP-LC) method was successfully validated and tested for the encapsulation efficiency assay of insulin and in vitro release studies. HPLC analyses were carried out using a RP C18- Luna® Phenomenex (4.6 × 250 mm, 5 μm particle size) column maintained at room temperature, using a mobile phase constituted by a mixture of acetonitrile and 0.1% TFA aqueous solution (60:40, v/v), in an isocratic mode with a flow rate of 1.0 mL/min, with ultraviolet detection at 214 nm and 20 μL of injection volume. Method validation was performed according recognized guidelines for system suitability, specificity, linearity, precision, accuracy, LOD, LOQ and robustness. The method was shown to be linear in the range of 0.5–100 μg/mL (r2 = 0.9993) selective, precise, robust, accurate with LOD and LOQ values were 0.097 μg/mL and 0.294 μg/mL, respectively. The developed method proved to be adequate to analyze the encapsulation efficiency and the profile of insulin release from liposomes.

Pharmacia ◽  
2020 ◽  
Vol 67 (2) ◽  
pp. 49-54
Author(s):  
Krassimira Yoncheva ◽  
Nadia Hristova-Avakumova ◽  
Vera Hadjimitova ◽  
Trayko Traykov ◽  
Petar Petrov

The study was focused on the evaluation of two copolymers as micellar carriers for kaempferol delivery. The copolymers comprised identical hydrophilic blocks of poly(2-(dimethylamino)ethyl methacrylate and different hydrophobic blocks of either poly(ε-caprolactone) (PDMAEMA9-b-PCL70-b-PDMAEMA9) or poly(propylene oxide) (PDMAEMA13-b-PPO69-b-PDMAEMA13). The calculation of Flory-Huggins parameters and determination of encapsulation efficiency showed that PDMAEMA-b-PCL-b-PDMAEMA copolymer possessed higher capacity for kaempferol loading. The diameter of the micelles before and after lyophilization was not changed, suggesting that the micelles could be lyophilized and redispersed before administration. The in vitro release of kaempferol from PDMAEMA-b-PPO-b-PDMAEMA micelles was faster than the release from PDMAEMA-b-PCL-b-PDMAEMA micelles, probably due to the higher affinity of kaempferol to this copolymer. Further, the higher affinity resulted in a retention of antioxidant activity of kaempferol in the presence of DPPH and KO2 radicals. Thus, PDMAEMA-PCL-PDMAEMA was considered more appropriate carrier because of the higher encapsulation efficiency and preservation of antioxidant activity of the drug.


Biomolecules ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 432
Author(s):  
Enkelejda Goci ◽  
Entela Haloci ◽  
Antonio Di Stefano ◽  
Annalisa Chiavaroli ◽  
Paola Angelini ◽  
...  

(1) Background: Capsaicin is the main capsaicinoid of the Capsicum genus and it is responsible for the pungent taste. Medical uses of the fruits of chili peppers date from the ancient time until nowadays. Most of all, they are used topically as analgesic in anti-inflammatory diseases as rheumatism, arthritis and in diabetic neuropathy. Reports state that the Capsicum genus, among other plant genera, is a good source of antimicrobial and antifungal compounds. The aim of this study was the preparation of a pharmaceutical Carbopol-based formulation containing capsaicin and the evaluation of its in vitro release and antimicrobial and antifungal properties. (2) Methods: It was first stabilized with an extraction method from the Capsicum annuum fruits with 98% ethanol and then the identification and determination of Capsaicin in this extract was realized by HPLC. (3) Results and Conclusions: Rheological analyses revealed that the selected formulation exhibited a pseudo-plastic behavior. In vitro release studies of capsaicin from a Carbopol-based formulation reported that approximately 50% of capsaicin was release within 52 h. Additionally, the Carbopol-based formulation significantly increased the antimicrobial effects of capsaicin towards all tested bacteria and fungi strains.


Clay Minerals ◽  
2011 ◽  
Vol 46 (4) ◽  
pp. 613-619 ◽  
Author(s):  
M. Betsiou ◽  
G. Bantsis ◽  
I. Zoi ◽  
C. Sikalidis

AbstractThis investigation was carried out to determine whether the adsorptive and ion-exchange properties of faujasite (FAU) could be used to delivery locally the anticancer drugs gemcitanine hydrochloride (dFdU.HCl) and oxaliplatin (DACH-Pt). A soaking procedure was used for the determination of the maximum adsorption capacity of FAU and the mechanism described here was achieved. 274 mg dFdU.HCl/g FAU were adsorbed in 16 h, while 48 h were needed for the adsorption of 79.7 mg DACH-Pt/g FAU. Drug release studies were carried out by soaking the samples of loaded FAU in simulation body fluids (SBF). After only one hour 76% of dFdU.HCl was released while the release of DACH-Pt from the FAU was more normal since 38% of DACH-Pt was released in the first 24 h.


2015 ◽  
Vol 1118 ◽  
pp. 28-36 ◽  
Author(s):  
Chao Long Ma ◽  
Cai Biao Hu ◽  
Shi Lei Ni ◽  
Ai Rui Qian ◽  
Qiang Xia

The aim of the present study was to prepare nanostructured lipid carriers (NLCs) and nanoemulsions (NEs) with different lipid compositions for delivery of phenylethyl resorcinol (PR) and investigate the effect of the lipid composition on the performance of lipid-based nanocarriers. The optimized nanocarriers were evaluated by photon correlation spectroscopy (PCS), Laser diffraction (LD), encapsulation efficiency, in vitro release and in vitro penetration studies. The particle sizes of all the freshly prepared nanocarriers were in the range of 70-200 nm. PR-NLCs showed higher encapsulation efficiency than PR-NEs. A controlled-release behavior of PR-NLCs was observed in in vitro release studies. In vitro penetration studies demonstrated nanocarriers with smaller particles possessed higher penetration ability. According to the present study, nanocarriers with small particle sizes can be considered as a potential drug delivery system for typical application.


2013 ◽  
Vol 2 (12) ◽  
pp. 196-201 ◽  
Author(s):  
Balagani Pavan Kumar ◽  
Irisappan Sarath Chandiran ◽  
Korlakunta Narasimha Jayaveera

The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion – solvent evaporation method. Microparticles were prepared using Eudragit RLPO by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines. The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 134.49 – 179.72 µm and encapsulation efficiency ranges from 92.30-98.32%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 hrs. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type. Eudragit RLPO microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.DOI: http://dx.doi.org/10.3329/icpj.v2i12.17016 International Current Pharmaceutical Journal, November 2013, 2(12): 196-201


Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.


2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.


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