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Diffusion barriers of tripartite sporopollenin microcapsules prepared from pine pollen.

ABSTRACT: Tripartite sporopollenin microcapsules prepared from pine pollen (Pinus sylvestris L. and Pinus nigra Arnold) were analysed with respect to the permeability of the different strata of the exine which surround the gametophyte and form the sacci. The sexine at the surface of the sacci is highly permeable for polymer molecules and latex particles with a diameter of up to 200 nm, whereas the nexine covering the gametophyte is impermeable for dextran molecules, with a Stokes' radius > or =4 nm (Dextran T 70), and for the tetravalent anionic dye Evans Blue (Stokes' radius = 1.3 nm). The central capsules obtained by dissolution of the sporoplasts showed strictly membrane-controlled exchange of non-electrolytes, with half-equilibration times in the range of minutes (monosaccharides, oligosaccharides) to hours (dextran molecules with Stokes' radii up to 2.5 nm). The dependence of the permeability coefficients of the nexine for non-electrolytes on Stokes' radius or molecular weight shows that the aqueous pores through the nexine are inhomogeneous with respect to their size, and that most pores are too narrow for free diffusion of sugar molecules. To explain the barrier function of the nexine for Evans Blue, it is assumed that at least the larger pores, which enable slow permeation of dextran molecules, contain negative charges.

SUBMITTER: Bohne G

PROVIDER: S-EPMC4243658 | biostudies-literature | 2003 Aug

REPOSITORIES: biostudies-literature

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Diffusion barriers of tripartite sporopollenin microcapsules prepared from pine pollen.

Bohne G G Richter E E Woehlecke H H Ehwald R R

Annals of botany 20030801 2

Tripartite sporopollenin microcapsules prepared from pine pollen (Pinus sylvestris L. and Pinus nigra Arnold) were analysed with respect to the permeability of the different strata of the exine which surround the gametophyte and form the sacci. The sexine at the surface of the sacci is highly permeable for polymer molecules and latex particles with a diameter of up to 200 nm, whereas the nexine covering the gametophyte is impermeable for dextran molecules, with a Stokes' radius > or =4 nm (Dextr ...[more]

PMID: 12876191

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Project description:Smart drug delivery systems (SDDSs) are a paradigm shift in drug delivery, particularly in microencapsulation technology where the drug is released in response to an internal and/or external stimulus. In this study, a smart microencapsulation platform was developed using three different types of stimuli triggered release of a model active (rhodamine 6G) from sporopollenin from Lycopodium clavatum. Triggers were based on pH-, thermal- and near infrared light-sensitive polymer composition. Carbopol nanogel and methylcellulose were used as responsive aqueous polymers for pH and thermally triggered release, respectively. Methylcellulose loaded with active and gold nanoparticles was used for photothermal triggered release. The formulations were encapsulated into the empty cores of sporopollenin microcapsules using the compressed tablet technique. The pH triggered release of the active was achieved above pH 7, which was mediated by the swelling of the carbopol nanogel that forced its way out of the elastic trilite scars of the sporopollenin. Results from measuring the active fluorescent intensity and its content over time confirmed the crucial role of carbopol in the pH triggered release. For the thermo-sensitive polymer methylcellulose, it was found that the release of the active from methylcellulose loaded sporopollenin was triggered upon heating the system reaching 90% whereas it levelled out at 40% for methylcellulose-free sporopollenin. The maximum amount of active was released at around 55 °C, where the sol-gel transition of the methylcellulose starts. Photothermally triggered release using near infrared (NIR) laser revealed that the amount of active released from sporopollenin loaded with both gold nanoparticles and methylcellulose was approximately four times higher than that from sporopollenin loaded with methylcellulose/active only, confirming the key role of gold nanoparticles in the release via photothermal heating of the polymer formulation.

Project description:We developed a dual microencapsulation platform for the type 2 diabetes drug metformin (MTF), which is aimed to increase its bioavailability. We report the use of Lycopodium clavatum sporopollenin (LCS), derived from their natural spores, and raw Phoenix dactylifera L. (date palm) pollens (DPP) for MTF microencapsulation. MTF was loaded into LCS and DPP via a vacuum and a novel method of hydration-induced swelling. The loading capacity (LC) and encapsulation efficiency (EE) percentages for MTF-loaded LCS and MTF-loaded DPP microcapsules were 14.9% ± 0.7, 29.8 ± 0.8, and 15.2% ± 0.7, 30.3 ± 1.0, respectively. The release of MTF from MTF-loaded LCS microcapsules was additionally controlled by re-encapsulating the loaded microcapsules into calcium alginate (ALG) microbeads via ionotropic gelation, where the release of MTF was found to be significantly slower and pH-dependent. The pharmacokinetic parameters, obtained from the in vivo study, revealed that the relative bioavailability of the MTF-loaded LCS-ALG beads was 1.215 times higher compared to pure MTF, following oral administration of a single dose equivalent to 25 mg/kg body weight MTF to streptozotocin (STZ)-induced diabetic male Sprague-Dawley rats. Significant hypoglycemic effect was obtained for STZ-induced diabetic rats orally treated with MTF-loaded LCS-ALG beads compared to control diabetic rats. Over a period of 29 days, the STZ-induced diabetic rats treated with MTF-loaded LCS-ALG beads showed a decrease in the aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglycerides, cholesterol, and low-density lipoprotein-cholesterol (LDL-C) levels, as well as an increase in glutathione peroxidase (GPx) and a recovery in the oxidative stress biomarker, lipid peroxidation (LPx). In addition, histopathological studies of liver, pancreas, kidney, and testes suggested that MTF-loaded LCS-ALG beads improved the degenerative changes in organs of diabetic rats. The LCS-ALG platform for dual encapsulation of MTF achieved sustained MTF delivery and enhancement of bioavailability, as well as the improved biochemical and histopathological characteristics in in vivo studies, opening many other intriguing applications in sustained drug delivery.

Dataset Information

Diffusion barriers of tripartite sporopollenin microcapsules prepared from pine pollen.

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Diffusion barriers of tripartite sporopollenin microcapsules prepared from pine pollen.

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