scholarly journals Morphology and Release Kinetics of Protein-Loaded Porous Poly(L-Lactic Acid) Spheres Prepared by Freeze-Drying Technique

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Takashi Sasaki ◽  
Kazuki Tanaka ◽  
Daisuke Morino ◽  
Kensuke Sakurai

Freeze-drying a biodegradable polymer, poly(L-lactic acid) (PLLA), from 1,4-dioxane solutions provided very porous spherical particles of ca. 3 mm in radius with specific surface area of 8–13 m2 g−1. The surface of the particle was found to be less porous compared with its interior. To apply the freeze-dried PLLA (FDPLLA) to drug delivery system, its morphology and drug releasing kinetics were investigated, bovine serum albumin (BSA) being used as a model drug compound. Immersion of FDPLLA into a BSA aqueous solution gave BSA-loaded FDPLLA, where mass fraction of the adsorbed BSA reached up to 79%. Time-dependent release profile of BSA in water suggested a two-step mechanism: (1) very rapid release of BSA deposited on and near the particle surface, which results in an initial burst, and (2) leaching of BSA from the interior of the particle by the diffusion process. It was suggested that the latter process is largely governed by the surface porosity. The porosity of both the interior and surface was found to decrease remarkably as the concentration of the original PLLA/1,4-dioxane solution increases, C0. Thus, C0 is a key parameter that controls the loading and releasing of BSA.

2015 ◽  
Vol 89 (1) ◽  
pp. 128-136
Author(s):  
Rareș Iuliu Iovanov ◽  
Ioan Tomuță ◽  
Sorin Emilian Leucuța

Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models. 


Materials ◽  
2019 ◽  
Vol 12 (12) ◽  
pp. 1924 ◽  
Author(s):  
Vojtech Kundrat ◽  
Nicole Cernekova ◽  
Adriana Kovalcik ◽  
Vojtech Enev ◽  
Ivana Marova

Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.


2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Takashi Sasaki ◽  
Hiroaki Matsuura ◽  
Kazuki Tanaka

Porous polymer spheres are promising materials as carriers for controlled drug release. As a new drug-carrier material, blend particles composed of poly(L-lactic acid) (PLLA) and rifampicin were developed using the freeze-drying technique. The blend particles exhibit high porosity with a specific surface area of 10–40 m2 g−1. Both the size and porosity of the particles depend on the concentration of the original solution and on the method of freezing. With respect to the latter, we used the drop method (pouring the original solution dropwise into liquid nitrogen) and the spray method (freezing a mist of the original solution). The release kinetics of rifampicin from the blend particles into water depends significantly on the morphology of the blend particles. The results show that the release rate can be controlled to a great extent by tuning the size and porosity of the blend particles, both of which are varied by parameters such as the solution concentration and the method of freezing.


2015 ◽  
Vol 365 ◽  
pp. 11-16
Author(s):  
R.J. Brandão ◽  
M.M. Prado ◽  
L.G. Marques

The freeze-drying rate is essentially low, since it is controlled by internal moisture diffusion. In addition, the application of vacuum and low temperature during the process presents a higher energy demand. Therefore, the search for new strategies to improve water mobility during freeze-drying constitutes a topic of relevant research. The aim of this work was to evaluate the use of power ultrasound to improve freeze-drying characteristics of açai, quantifying the influence of the applied power on both the drying and rehydration kinetics of the material. Açai (Euterpe oleracea Martius) samples were sonicated with two different frequency levels, 20 kHz and 40 kHz, and two sonication times, 3 min and 10 min. Page’s equation considering internal and external resistances to mass transfer provided a good fit of freeze-drying kinetics, while the Peleg’s equation was found to be suitable for describing the rehydration kinetics of freeze-dried açai. Pretreatment of açai with ultrasound waves was not effective. Ultrasound-induced structural disruption in the açai skin hindered the mass transfer during both freeze-drying and rehydration processes.


RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16167-16175 ◽  
Author(s):  
Shiping Zhan ◽  
Jingchang Wang ◽  
Weijing Wang ◽  
Liyun Cui ◽  
Qicheng Zhao

In this work, drug-loaded polymer microparticles were prepared by a supercritical solution impregnation (SSI) process with nitrendipine as the model drug and PLLA–PEG–PLLA as the drug carrier.


2010 ◽  
Vol 60 (4) ◽  
pp. 373-385 ◽  
Author(s):  
Tina Ukmar ◽  
Odon Planinšek

Ordered mesoporous silicates as matrices for controlled release of drugs Interest in and thereby also development of ordered mesoporous silicates as drug delivery devices have grown immensely over the past few years. On hand selected cases from the literature, the power of such systems as delivery devices has been established. Specifically, it is shown how it is possible to enhance the release kinetics of poorly soluble drugs by embedding them in mesoporous silicates. Further critical factors governing the structure and release of the model drug itraconazole incorporated in an SBA-15 matrix are briefly reviewed. The possibility of functionalizing the surface of mesoporous matrices also under harsher conditions offers a broad platform for the design of stimuli-responsive drug release, including pH responsive systems and systems which respond to the presence of specific ions, reducing agents, magnetic field or UV light, whose efficiency and biocompatibility has been established in vitro.


1974 ◽  
Vol 20 (11) ◽  
pp. 1529-1534 ◽  
Author(s):  
C. S. Cox ◽  
S. J. Gagen ◽  
Jean Baxter

Previously the kinetics of loss of viability of freeze-dried Serratia marcescens 8UK were determined by Cox and Heckly as a function of oxygen concentration and time. Results are presented here when dehydration is brought about by aerosolization into atmospheres of low relative humidity (RH) rather than by freeze-drying. As for freeze-dried S. marcescens, oxygen was toxic and viable decay followed the same kinetics with respect to oxygen concentration and time. The influence of RH upon viable decay (which was not studied in the previous report) was that above 65% RH oxygen was not toxic but was progressively more toxic as the humidity was further reduced. Kinetic analyses of the results indicate that the site for the toxic action of oxygen lies in the interspace between the cytoplasmic membrane and the cell wall. Such a finding is consistent with other data which suggest that cell division and (or) cell wall synthesis in bacteria are inhibited by oxygen.


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