Chitosan-based nanoparticles for rosmarinic acid ocular delivery—In vitro tests

Silva, Sara Baptista da; Ferreira, Domingos; Pintado, Manuela; Sarmento, Bruno

doi:10.1016/j.ijbiomac.2015.11.070

Cited by 122 publications

(72 citation statements)

References 78 publications

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“…The results of this study revealed the great merit of CA nanofibers as RosA delivery patches compared to the previously reported polymer‐based RosA delivery systems. The loading efficiency of 40–60% and the fast initial release of around 90–100% of RosA in 30–45 min that were reported for chitosan micro/nanoparticle‐based RosA delivery systems prepared by ionic gelation or spray drying might be due to association of RosA with particles on their surfaces by weak linkages .…”

Section: Discussionmentioning

confidence: 82%

“…Although incorporation of RosA in micro/nanoparticles for biomedical and cosmetic applications were recently reported by many researchers [5,19,20,[42][43][44][45][46][47], this is the preliminary attempt to entrap RosA within a nanofibrous matrix and to study the potential of RosA-loaded nanofibers as a drug delivery system with anti-inflammatory and antioxidant properties.…”

Section: Discussionmentioning

confidence: 99%

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Rosmarinic acid‐loaded electrospun nanofibers: In vitro release kinetic study and bioactivity assessment

Vatankhah

2018

Engineering in Life Sciences

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This study seeks to develop a nanofibrous matrix containing rosmarinic acid (RosA), an herbal non‐steroidal anti‐inflammatory and antioxidant drug with low water solubility, for drug delivery applications. Neat and two types of RosA‐loaded cellulose acetate (CA) mats varying in the initial content of RosA were electrospun. Microstructure of nanofibers, chemistry and physical state of RosA in nanofibers, RosA loading efficiency and RosA release in acetate buffer were investigated. To evaluate bioactivity of RosA‐loaded nanofibers, their ability to inhibit protein denaturation was assayed as an indicator of anti‐inflammatory properties and their antioxidant activity was determined by radical scavenging assay. The indirect cytotoxicity assay was used to find if there is a cytotoxic response to nanofibers. The homogeneous distribution of the drug within nanofibers through electrospinning led to high loading efficiency, low burst release and prolonged release of a large percentage of RosA over a period of 64h following Fickian diffusion mechanism. Nanofibers with higher RosA content exhibited anti‐inflammatory activity comparable to ibuprofen, and higher antioxidant activity compared to nanofibers with lower RosA content. Additionally, extracts from nanofibers did not give any major harmful effect on cells. Sustained release of RosA, and bioactivity of RosA‐loaded nanofibers confirmed the potential of the produced matrix as a drug delivery system.

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Section: Discussionmentioning

confidence: 82%

Section: Discussionmentioning

confidence: 99%

Rosmarinic acid‐loaded electrospun nanofibers: In vitro release kinetic study and bioactivity assessment

Vatankhah

2018

Engineering in Life Sciences

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“…The permeability of rosmarinic acid facilitated by the NP formulation was found to be significantly higher compared to free solution. Mucoadhesion studies reveal that the NPs interact with the ocular mucosa [93]. Imiquimod was formulated as both chitosan coated PCL nanocapsules embedded in hydroethylcellulose gel and PCL nanocapsules embedded in chitosan hydrogel for vaginal delivery to treat human papillomavirus infection [94].…”

Section: Mucoadhesionmentioning

confidence: 99%

An Overview of Chitosan Nanoparticles and Its Application in Non-Parenteral Drug Delivery

et al. 2017

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The focus of this review is to provide an overview of the chitosan based nanoparticles for various non-parenteral applications and also to put a spotlight on current research including sustained release and mucoadhesive chitosan dosage forms. Chitosan is a biodegradable, biocompatible polymer regarded as safe for human dietary use and approved for wound dressing applications. Chitosan has been used as a carrier in polymeric nanoparticles for drug delivery through various routes of administration. Chitosan has chemical functional groups that can be modified to achieve specific goals, making it a polymer with a tremendous range of potential applications. Nanoparticles (NP) prepared with chitosan and chitosan derivatives typically possess a positive surface charge and mucoadhesive properties such that can adhere to mucus membranes and release the drug payload in a sustained release manner. Chitosan-based NP have various applications in non-parenteral drug delivery for the treatment of cancer, gastrointestinal diseases, pulmonary diseases, drug delivery to the brain and ocular infections which will be exemplified in this review. Chitosan shows low toxicity both in vitro and some in vivo models. This review explores recent research on chitosan based NP for non-parenteral drug delivery, chitosan properties, modification, toxicity, pharmacokinetics and preclinical studies.

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“…Numerous biological activities have been described for rosmarinic acid, such as astringent, antioxidative, anti-inflammatory, antimutagenic, antibacterial, and antiviral [1]. The antioxidant activity of rosmarinic acid is related to its antiangiogenic activity by the inhibition of important steps of angiogenesis, including prolif-eration, migration, and adhesion in a concentration-dependent manner [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Rosmarinic Acid Intravitreal Implants: A New Therapeutic Approach for Ocular Neovascularization

et al. 2020

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Rosmarinic acid, a plant-derived compound with antiangiogenic activity, can be applied for the treatment of ocular diseases related to neovascularization, such as diabetic retinopathy, macular edema, and age-related macular degeneration. These diseases represent the leading causes of blindness worldwide if they are not properly treated. Intravitreal devices allow for localized drug delivery to the posterior segment, increasing the drug bioavailability and promoting extended release, thus, reducing side effects and enhancing the patientʼs compliance to the treatment. In this work, rosmarinic acid-loaded poly lactic-co-glycolic acid intraocular implants were developed with a view for the treatment of ocular neovascularization. Physical-chemical, biocompatibility, and safety studies of the implants were carried out in vitro and in vivo as well as an evaluation of the antiangiogenic activity in a chorioallantoic membrane assay. Data obtained showed that rosmarinic acid released from the implants was quantified in the vitreous for 6 weeks, while when it was in the solution formulation, after 24 h, no drug was found in the vitreous. The delivery device did not show any sign of toxicity after clinical evaluation and in electroretinographic findings. Histological analysis showed normal eye tissue. Rosmarinic acid released from implants reduced 30% of new vesselʼs formation. The intravitreal implant successfully allowed for the prolonged release of rosmarinic acid, was safe to rabbits eyes, and demonstrated activity in vessel reduction, thus demonstrating potential in preventing neovascularization in ophthalmic diseases.

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Chitosan-based nanoparticles for rosmarinic acid ocular delivery—In vitro tests

Cited by 122 publications

References 78 publications

Rosmarinic acid‐loaded electrospun nanofibers: In vitro release kinetic study and bioactivity assessment

Rosmarinic acid‐loaded electrospun nanofibers: In vitro release kinetic study and bioactivity assessment

An Overview of Chitosan Nanoparticles and Its Application in Non-Parenteral Drug Delivery

Rosmarinic Acid Intravitreal Implants: A New Therapeutic Approach for Ocular Neovascularization

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