Comparative analysis of PLGA ocuserts of brimonidine tartrate prepared with different methods

Abstract The eye is a highly sensitive organ with multiple physiological barriers that limit drug bioavailability and reduce patient compliance. Research studies are still going on to discover a novel drug delivery system for ocular delivery. The current research aims to develop and compare the PLGA ocuserts of brimonidine tartrate (BT) by different methods. These BT-loaded PLGA ocuserts offer a promising alternative to commercially available BT eye drops. Ocuserts could significantly minimize the challenges encountered with eye drops like lacrimation, blinking-induced washout, dosing frequency, penetration, stability, and controlled release issues. The BT-loaded PLGA ocuserts were prepared using two methods: solvent casting method (SCM) and glass substrate method (GSM). Both SCM and GSM formulations exhibited smooth texture, pH levels within the range of 6.88±0.24 to 6.90±0.28, uniform thickness (SCM: 0.47±0.10 mm; GSM: 0.29±0.03 mm), minimal weight variation (SCM: 7.83±0.38 mg; GSM: 6.55±0.76 mg), sterility, and appropriate swelling indices (SCM: 6.69±0.33%; GSM: 5.40±0.27%). The evaluation results of SCM and GSM ocuserts revealed positive attributes for ophthalmic use. Noteworthy distinctions emerged in folding endurance, with SCM ocuserts demonstrating significantly higher endurance (87.17±4.34 folds) than GSM ocuserts (71.33±4.82 folds). Moreover, SCM ocuserts exhibited superior drug entrapment efficiency (88.26±3.33 %) to GSM ocuserts (74.91±4.39 %). Stability studies confirmed good stability over a 6-month period, while in vitro (italics) drug release study indicated better controlled release properties for SCM than GSM. Findings demonstrate that SCM emerged as an effective method for preparation of polymeric films in various pharmaceutical industries, including transdermal patches, scaffolds in tissue engineering, flexible wound healing films, biodegradable drug delivery systems, and pharmaceutical packaging as well.

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Publication Details

Journal
European Pharmaceutical Journal
Published
2025-05-17
DOI
https://doi.org/10.2478/afpuc-2025-0001
Primary Topic
Ocular Surface and Contact Lens
Type
article
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article

Comparative analysis of PLGA ocuserts of brimonidine tartrate prepared with different methods

Bimlesh Kumar, Paramjot, Dileep Singh Baghel, Sheetu Wadhwa et al.
European Pharmaceutical Journal
Ocular Surface and Contact Lens
article

Comparative analysis of PLGA ocuserts of brimonidine tartrate prepared with different methods

Bimlesh Kumar, Paramjot, Dileep Singh Baghel, Sheetu Wadhwa, Saurabh Singh
article en

Abstract

Abstract The eye is a highly sensitive organ with multiple physiological barriers that limit drug bioavailability and reduce patient compliance. Research studies are still going on to discover a novel drug delivery system for ocular delivery. The current research aims to develop and compare the PLGA ocuserts of brimonidine tartrate (BT) by different methods. These BT-loaded PLGA ocuserts offer a promising alternative to commercially available BT eye drops. Ocuserts could significantly minimize the challenges encountered with eye drops like lacrimation, blinking-induced washout, dosing frequency, penetration, stability, and controlled release issues. The BT-loaded PLGA ocuserts were prepared using two methods: solvent casting method (SCM) and glass substrate method (GSM). Both SCM and GSM formulations exhibited smooth texture, pH levels within the range of 6.88±0.24 to 6.90±0.28, uniform thickness (SCM: 0.47±0.10 mm; GSM: 0.29±0.03 mm), minimal weight variation (SCM: 7.83±0.38 mg; GSM: 6.55±0.76 mg), sterility, and appropriate swelling indices (SCM: 6.69±0.33%; GSM: 5.40±0.27%). The evaluation results of SCM and GSM ocuserts revealed positive attributes for ophthalmic use. Noteworthy distinctions emerged in folding endurance, with SCM ocuserts demonstrating significantly higher endurance (87.17±4.34 folds) than GSM ocuserts (71.33±4.82 folds). Moreover, SCM ocuserts exhibited superior drug entrapment efficiency (88.26±3.33 %) to GSM ocuserts (74.91±4.39 %). Stability studies confirmed good stability over a 6-month period, while in vitro (italics) drug release study indicated better controlled release properties for SCM than GSM. Findings demonstrate that SCM emerged as an effective method for preparation of polymeric films in various pharmaceutical industries, including transdermal patches, scaffolds in tissue engineering, flexible wound healing films, biodegradable drug delivery systems, and pharmaceutical packaging as well.

European Pharmaceutical JournalVol. 72(1)
Lovely Professional University (IN)
Openalex Percentile: Top 85%
Ocular Surface and Contact Lens
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