Encapsulation of erythromycin and bacitracin antibiotics into natural sporopollenin microcapsules: antibacterial, cytotoxicity,<i>in vitro</i>and<i>in vivo</i>release studies for enhanced bioavailability

Dyab, Amro K. F.; Mohamed, Mohamed A.; Meligi, Noha M.; Mohamed, Shaaban K.

doi:10.1039/c8ra05499a

Cited by 35 publications

(20 citation statements)

References 66 publications

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“…Interestingly, it was revealed that sporopollenin of Lycopodium clavatum formulated with ovalbumin, a model antigen, stimulated a “systemic and a mucosal immune response” following oral administration to mice [ 76 ]. Required for industrial applications, the biocompatibility and biodegradability of sporopollenin extracted from Lycopodium clavatum have been proven in several studies [ 52 , 53 , 56 , 74 , 77 ].…”

Section: Resultsmentioning

confidence: 99%

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

2021

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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.

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Section: Resultsmentioning

confidence: 99%

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

2021

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“…The drug-filled microcapsules have been found to be effectual for human colon carcinoma cell line via MTT assay [ 40 ]. In another study, the sporopollenin isolated from Lycopodium clavatum spores was utilized for the encapsulation of erythromycin and bacitracin antibiotics [ 41 ]; the entrapment and filling competence of erythromycin were 32.4% and 16.2, respectively. The activities of antibiotic-loaded sporopollenin, pure antibiotics, and unfilled sporopollenin have been evaluated against Pseudomonas aeruginosa , Staphylococcus aureus , and Klebsiella pneumoniae .…”

Section: Drug Delivery Applicationsmentioning

confidence: 99%

“…A deviation from Fick's law was illustrated by the in vitro discharge mechanism for erythromycin at pH 7.4. I The discharge of erythromycin in vivo from sporopollenin (oral dosage 50 mg kg −1 ) showed remarkable values displaying the improved bioavailability of erythromycin [ 41 ].…”

Section: Drug Delivery Applicationsmentioning

confidence: 99%

Plant Pollen Grains: A Move Towards Green Drug and Vaccine Delivery Systems

Iravani

Varma

2021

Nano-Micro Lett.

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Pollen grains and plant spores have emerged as innovative biomaterials for various applications such as drug/vaccine delivery, catalyst support, and the removal of heavy metals. The natural microcapsules comprising spore shells and pollen grain are designed for protecting the genetic materials of plants from exterior impairments. Two layers make up the shell, the outer layer (exine) that comprised largely of sporopollenin, and the inner layer (intine) that built chiefly of cellulose. These microcapsule shells, namely hollow sporopollenin exine capsules have some salient features such as homogeneity in size, non-toxic nature, resilience to both alkalis and acids, and the potential to withstand at elevated temperatures; they have displayed promising potential for the microencapsulation and the controlled drug delivery/release. The important attribute of mucoadhesion to intestinal tissues can prolong the interaction of sporopollenin with the intestinal mucosa directing to an augmented effectiveness of nutraceutical or drug delivery. Here, current trends and prospects related to the application of plant pollen grains for the delivery of vaccines and drugs and vaccine are discussed. "Image missing"

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“…These unique properties have already drawn researchers’ attention [ 2 ]; notwithstanding, it is well known that most pollens contain allergens that constitute a potential risk to human health [ 1 , 9 ]. A few protocols have already been established for the elimination of such components and/or the chemical extraction of sporopollenin from fern spores and pollen grains [ 10 , 11 , 12 ] to encapsulate drugs [ 13 , 14 ], lipids [ 15 ], cells [ 16 ], proteins [ 17 , 18 ], or chemical catalysts [ 19 , 20 ]. Such procedures usually involve laborious processes using harsh reagents (e.g., strong acids and/or bases) and prolonged incubation times that can alter the ultrastructure of the pollen grain [ 10 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

Purification of Hollow Sporopollenin Microcapsules from Sunflower and Chamomile Pollen Grains

et al. 2021

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Pollen grains are natural microcapsules comprised of the biopolymer sporopollenin. The uniformity and special tridimensional architecture of these sporopollenin structures confer them attractive properties such as high resistance and improved bioadhesion. However, natural pollen can be a source of allergens, hindering its biomedical applicability. Several methods have been developed to remove internal components and allergenic compounds, usually involving long and laborious processes, which often cannot be extended to other pollen types. In this work, we propose an abridged protocol to produce stable and pristine hollow pollen microcapsules, together with a complete physicochemical and morphological characterization of the intermediate and final products. The optimized procedure has been validated for different pollen samples, also producing sporopollenin microcapsules from Matricaria species for the first time. Pollen microcapsules obtained through this protocol presented low protein content (4.4%), preserved ornamented morphology with a nanoporous surface, and low product density (0.14 g/cm3). These features make them interesting candidates from a pharmaceutical perspective due to the versatility of this biomaterial as a drug delivery platform.

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Encapsulation of erythromycin and bacitracin antibiotics into natural sporopollenin microcapsules: antibacterial, cytotoxicity,in vitroandin vivorelease studies for enhanced bioavailability

Abstract: Antibacterial activity and bioavailability of antibiotics are enhanced after a successful loading into nontoxic natural Lycopodium clavatum sporopollenin microcapsules.

Cited by 35 publications

References 66 publications

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

Sustained In Vitro and In Vivo Delivery of Metformin from Plant Pollen-Derived Composite Microcapsules

Plant Pollen Grains: A Move Towards Green Drug and Vaccine Delivery Systems

Purification of Hollow Sporopollenin Microcapsules from Sunflower and Chamomile Pollen Grains

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