Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin

Age-related macular degeneration is a multifactorial disease affecting the posterior segment of the eye and is characterized by aberrant nascent blood vessels that leak blood and fluid. It ends with vision loss. In the present study, artemisinin which is poorly water-soluble and has potent anti-angi...

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Main Authors: Chandrasekar Ponnusamy, Abimanyu Sugumaran, Venkateshwaran Krishnaswami, Rajaguru Palanichamy, Ravichandiran Velayutham, Subramanian Natesan
Format: Article
Language:English
Published: MDPI AG 2021-09-01
Series:Polymers
Subjects:
Online Access:https://www.mdpi.com/2073-4360/13/18/3038
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author Chandrasekar Ponnusamy
Abimanyu Sugumaran
Venkateshwaran Krishnaswami
Rajaguru Palanichamy
Ravichandiran Velayutham
Subramanian Natesan
author_facet Chandrasekar Ponnusamy
Abimanyu Sugumaran
Venkateshwaran Krishnaswami
Rajaguru Palanichamy
Ravichandiran Velayutham
Subramanian Natesan
author_sort Chandrasekar Ponnusamy
collection DOAJ
description Age-related macular degeneration is a multifactorial disease affecting the posterior segment of the eye and is characterized by aberrant nascent blood vessels that leak blood and fluid. It ends with vision loss. In the present study, artemisinin which is poorly water-soluble and has potent anti-angiogenic and anti-inflammatory properties was formulated into nanomicelles and characterized for its ocular application and anti-angiogenic activity using a CAM assay. Artemisinin-loaded nanomicelles were prepared by varying the concentrations of PVP k90 and poloxamer 407 at different ratios and showed spherical shape particles in the size range of 41–51 nm. The transparency and cloud point of the developed artemisinin-loaded nanomicelles was found to be 99–94% and 68–70 °C, respectively. The in vitro release of artemisinin from the nanomicelles was found to be 96.0–99.0% within 8 h. The trans-corneal permeation studies exhibited a 1.717–2.169 µg permeation of the artemisinin from nanomicelles through the excised rabbit eye cornea for 2 h. Drug-free nanomicelles did not exhibit noticeable DNA damage and showed an acceptable level of hemolytic potential. Artemisinin-loaded nanomicelles exhibited remarkable anti-angiogenic activity compared to artemisinin suspension. Hence, the formulated artemisinin-loaded nanomicelles might have the potential for the treatment of AMD.
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spelling doaj.art-54976c2317af48e0b95eb59b027edee12023-11-22T14:55:06ZengMDPI AGPolymers2073-43602021-09-011318303810.3390/polym13183038Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of ArtemisininChandrasekar Ponnusamy0Abimanyu Sugumaran1Venkateshwaran Krishnaswami2Rajaguru Palanichamy3Ravichandiran Velayutham4Subramanian Natesan5Department of Pharmaceutical Technology, University College of Engineering, Bharathidasan Institute of Technology Campus, Anna University, Tiruchirappalli 620024, Tamil Nadu, IndiaDepartment of Pharmaceutics, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur 603203, Tamil Nadu, IndiaDepartment of Pharmaceutical Technology, University College of Engineering, Bharathidasan Institute of Technology Campus, Anna University, Tiruchirappalli 620024, Tamil Nadu, IndiaDepartment of Life Sciences, School of Life Sciences, Central University of Tamil Nadu, Tiruvarur 627007, Tamil Nadu, IndiaDepartment of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)—Kolkata, Chunilal Bhawan, 168, Maniktala Main Road, Kolkata 700054, West Bengal, IndiaDepartment of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)—Kolkata, Chunilal Bhawan, 168, Maniktala Main Road, Kolkata 700054, West Bengal, IndiaAge-related macular degeneration is a multifactorial disease affecting the posterior segment of the eye and is characterized by aberrant nascent blood vessels that leak blood and fluid. It ends with vision loss. In the present study, artemisinin which is poorly water-soluble and has potent anti-angiogenic and anti-inflammatory properties was formulated into nanomicelles and characterized for its ocular application and anti-angiogenic activity using a CAM assay. Artemisinin-loaded nanomicelles were prepared by varying the concentrations of PVP k90 and poloxamer 407 at different ratios and showed spherical shape particles in the size range of 41–51 nm. The transparency and cloud point of the developed artemisinin-loaded nanomicelles was found to be 99–94% and 68–70 °C, respectively. The in vitro release of artemisinin from the nanomicelles was found to be 96.0–99.0% within 8 h. The trans-corneal permeation studies exhibited a 1.717–2.169 µg permeation of the artemisinin from nanomicelles through the excised rabbit eye cornea for 2 h. Drug-free nanomicelles did not exhibit noticeable DNA damage and showed an acceptable level of hemolytic potential. Artemisinin-loaded nanomicelles exhibited remarkable anti-angiogenic activity compared to artemisinin suspension. Hence, the formulated artemisinin-loaded nanomicelles might have the potential for the treatment of AMD.https://www.mdpi.com/2073-4360/13/18/3038nanomicellesartemisinincorneatoxicity
spellingShingle Chandrasekar Ponnusamy
Abimanyu Sugumaran
Venkateshwaran Krishnaswami
Rajaguru Palanichamy
Ravichandiran Velayutham
Subramanian Natesan
Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
Polymers
nanomicelles
artemisinin
cornea
toxicity
title Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
title_full Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
title_fullStr Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
title_full_unstemmed Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
title_short Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin
title_sort development and evaluation of polyvinylpyrrolidone k90 and poloxamer 407 self assembled nanomicelles enhanced topical ocular delivery of artemisinin
topic nanomicelles
artemisinin
cornea
toxicity
url https://www.mdpi.com/2073-4360/13/18/3038
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