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In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide.
Drug Deliv Transl Res. 2019 04; 9(2):534-542.DD

Abstract

The objectives of this study were to develop biodegradable poly-lactic-co-glycolic acid (PLGA) based injectable phase inversion in situ forming system for sustained delivery of triamcinolone acetonide (TA) and to conduct physicochemical characterisation including in vitro drug release of the prepared formulations. TA (at 0.5%, 1% and 2.5% w/w loading) was dissolved in N-methyl-2-pyrrolidone (NMP) solvent and then incorporated 30% w/w PLGA (50/50 and 75/25) polymer to prepare homogenous injectable solution. The formulations were evaluated for rheological behaviour using rheometer, syringeability by texture analyser, water uptake and rate of implant formation by optical coherence tomography (OCT) microscope. Phase inversion in situ forming formulations were injected into PBS pH 7.3 to form an implant and release samples were collected and analysed for drug content using a HPLC method. All formulations exhibited good syringeability and rheological properties (viscosity: 0.19-3.06 Pa.s) by showing shear thinning behaviour which enable them to remain as free-flowing solution for ease administration. The results from OCT microscope demonstrated that thickness of the implants were increased with the increase in time and the rate of implant formation indicated the fast phase inversion. The drug release from implants was sustained over a period of 42 days. The research findings demonstrated that PLGA/NMP-based phase inversion in situ forming implants can improve compliance in patient's suffering from ocular diseases by sustaining the drug release for a prolonged period of time and thereby reducing the frequency of ocular injections.

Authors+Show Affiliations

School of Pharmacy, International Medical University, 57000, Bukit Jalil, Kuala Lumpur, Malaysia. ravisheshala@uitm.edu.my. Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi MARA Selangor, Puncak Alam Campus, 42300, Puncak Alam, Kuala Selangor, Malaysia. ravisheshala@uitm.edu.my.School of Pharmacy, International Medical University, 57000, Bukit Jalil, Kuala Lumpur, Malaysia.School of Pharmacy, International Medical University, 57000, Bukit Jalil, Kuala Lumpur, Malaysia.School of Pharmacy, International Medical University, 57000, Bukit Jalil, Kuala Lumpur, Malaysia.School of Pharmacy, McClay Research Centre, Queens University Belfast, 97 Lisburn Road, Belfast, Northern Ireland, BT9 7BL, UK. r.thakur@qub.ac.uk.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

29484530

Citation

Sheshala, Ravi, et al. "In Situ Forming Phase-inversion Implants for Sustained Ocular Delivery of Triamcinolone Acetonide." Drug Delivery and Translational Research, vol. 9, no. 2, 2019, pp. 534-542.
Sheshala R, Hong GC, Yee WP, et al. In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide. Drug Deliv Transl Res. 2019;9(2):534-542.
Sheshala, R., Hong, G. C., Yee, W. P., Meka, V. S., & Thakur, R. R. S. (2019). In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide. Drug Delivery and Translational Research, 9(2), 534-542. https://doi.org/10.1007/s13346-018-0491-y
Sheshala R, et al. In Situ Forming Phase-inversion Implants for Sustained Ocular Delivery of Triamcinolone Acetonide. Drug Deliv Transl Res. 2019;9(2):534-542. PubMed PMID: 29484530.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide. AU - Sheshala,Ravi, AU - Hong,Gan Chew, AU - Yee,Wong Pui, AU - Meka,Venkata Srikanth, AU - Thakur,Raghu Raj Singh, PY - 2018/2/28/pubmed PY - 2019/8/14/medline PY - 2018/2/28/entrez KW - In situ implant KW - Ocular KW - PLGA KW - Phase inversion KW - Triamcinolone acetonide SP - 534 EP - 542 JF - Drug delivery and translational research JO - Drug Deliv Transl Res VL - 9 IS - 2 N2 - The objectives of this study were to develop biodegradable poly-lactic-co-glycolic acid (PLGA) based injectable phase inversion in situ forming system for sustained delivery of triamcinolone acetonide (TA) and to conduct physicochemical characterisation including in vitro drug release of the prepared formulations. TA (at 0.5%, 1% and 2.5% w/w loading) was dissolved in N-methyl-2-pyrrolidone (NMP) solvent and then incorporated 30% w/w PLGA (50/50 and 75/25) polymer to prepare homogenous injectable solution. The formulations were evaluated for rheological behaviour using rheometer, syringeability by texture analyser, water uptake and rate of implant formation by optical coherence tomography (OCT) microscope. Phase inversion in situ forming formulations were injected into PBS pH 7.3 to form an implant and release samples were collected and analysed for drug content using a HPLC method. All formulations exhibited good syringeability and rheological properties (viscosity: 0.19-3.06 Pa.s) by showing shear thinning behaviour which enable them to remain as free-flowing solution for ease administration. The results from OCT microscope demonstrated that thickness of the implants were increased with the increase in time and the rate of implant formation indicated the fast phase inversion. The drug release from implants was sustained over a period of 42 days. The research findings demonstrated that PLGA/NMP-based phase inversion in situ forming implants can improve compliance in patient's suffering from ocular diseases by sustaining the drug release for a prolonged period of time and thereby reducing the frequency of ocular injections. SN - 2190-3948 UR - https://www.unboundmedicine.com/medline/citation/29484530/In_situ_forming_phase_inversion_implants_for_sustained_ocular_delivery_of_triamcinolone_acetonide_ L2 - https://dx.doi.org/10.1007/s13346-018-0491-y DB - PRIME DP - Unbound Medicine ER -