Formulation, Development, and Characterization of AMB-Based Subcutaneous Implants using PCL and PLGA via Hot-Melt Extrusion
The hot-melt extrusion process is currently considered a prominent manufacturing technique in the pharmaceutical industry. The present study is intended to develop amlodipine besylate (AMB)-loaded subcutaneous implants to reduce the frequency of administration, thus improving patient compliance duri...
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| Veröffentlicht in: | AAPS PharmSciTech 2024-12, Vol.26 (1), p.16, Article 16 |
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| creator | Chitnis, Kshitij Narala, Nagarjuna Vemula, Sateesh Kumar Narala, Sagar Munnangi, Sivaram Repka, Michael A. |
| description | The hot-melt extrusion process is currently considered a prominent manufacturing technique in the pharmaceutical industry. The present study is intended to develop amlodipine besylate (AMB)-loaded subcutaneous implants to reduce the frequency of administration, thus improving patient compliance during hypertension management. AMB subcutaneous implants were prepared using continuous hot-melt extrusion technology using poly(caprolactone) and poly(lactic-co-glycolic acid) with dimensions of 3.70 cm (length) by 2.00 mm (diameter). The implants were characterized for thermal characteristics, drug-excipient incompatibilities, surface morphology, fracturability,
in vitro
drug release, and stability studies. Differential scanning calorimetry study confirmed the drug's crystalline state within the fabricated implants, while textural analysis demonstrated good fracturability in the lead formulation. Scanning electron microscopy revealed the smooth surface morphology of the lead subcutaneous implant. The lead formulation showed an extended drug release profile over 30 days (~ 2.25 mg per day) and followed zero-order release kinetics (R
2
value to 0.9999) with a mean dissolution time of 14.96 days. The lead formulation remained stable for 30 days at accelerated stability conditions of 40°C and 75% relative humidity. In conclusion, developing hot-melt extruded implants could be an alternative to the conventional amlodipine besylate (AMB) formulation.
Graphical Abstract |
| doi_str_mv | 10.1208/s12249-024-03004-4 |
| format | Article |
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in vitro
drug release, and stability studies. Differential scanning calorimetry study confirmed the drug's crystalline state within the fabricated implants, while textural analysis demonstrated good fracturability in the lead formulation. Scanning electron microscopy revealed the smooth surface morphology of the lead subcutaneous implant. The lead formulation showed an extended drug release profile over 30 days (~ 2.25 mg per day) and followed zero-order release kinetics (R
2
value to 0.9999) with a mean dissolution time of 14.96 days. The lead formulation remained stable for 30 days at accelerated stability conditions of 40°C and 75% relative humidity. In conclusion, developing hot-melt extruded implants could be an alternative to the conventional amlodipine besylate (AMB) formulation.
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in vitro
drug release, and stability studies. Differential scanning calorimetry study confirmed the drug's crystalline state within the fabricated implants, while textural analysis demonstrated good fracturability in the lead formulation. Scanning electron microscopy revealed the smooth surface morphology of the lead subcutaneous implant. The lead formulation showed an extended drug release profile over 30 days (~ 2.25 mg per day) and followed zero-order release kinetics (R
2
value to 0.9999) with a mean dissolution time of 14.96 days. The lead formulation remained stable for 30 days at accelerated stability conditions of 40°C and 75% relative humidity. In conclusion, developing hot-melt extruded implants could be an alternative to the conventional amlodipine besylate (AMB) formulation.
Graphical Abstract</description><subject>Amlodipine - administration & dosage</subject><subject>Amlodipine - chemistry</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Calorimetry, Differential Scanning - methods</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Delayed-Action Preparations - chemistry</subject><subject>Drug Compounding - methods</subject><subject>Drug Implants - chemistry</subject><subject>Drug Liberation</subject><subject>Drug Stability</subject><subject>Excipients - chemistry</subject><subject>Hot Melt Extrusion Technology - methods</subject><subject>Hot Temperature</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Polyesters - chemistry</subject><subject>Polylactic Acid-Polyglycolic Acid Copolymer - chemistry</subject><subject>Research Article</subject><subject>Solubility</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><recordid>eNp9kE1PGzEQhi3UCijlD3BAPvaA2_HHfvgYwkciBYHU9mw5XhsW7dqp7Y1a-PPdZgH1xGlGmmdezTwInVD4ShnU3xJlTEgCTBDgAIKIPXRICw5ESs4-_NcfoE8pPQIwTiXfRwdclhJ4JQ_R81WI_dDp3AZ_hi_s1nZh01ufz7D2DZ4_6KhNtrF92iE4ODy7OSfnOtkGfx_WZsja2zAkvOw3nfY54SG1_h7fzVe7hLvV9QxvW40XIZMb22V8-TvHkQn-M_rodJfs8Us9Qj-vLn_MF2R1e72cz1bEsIplwsEJp8vayEoLBhSMhrXRtSy1dE1hHS3roiok1BoqoI2zlBeC1cbxmlZryY_Qlyl3E8Ovwaas-jYZ23XT5YpTUUpRScpHlE2oiSGlaJ3axLbX8Y-ioP5JV5N0NUpXO-lKjEunL_nDurfN28qr5RHgE5DGkb-3UT2GIfrx5_di_wKBu4yO</recordid><startdate>20241217</startdate><enddate>20241217</enddate><creator>Chitnis, Kshitij</creator><creator>Narala, Nagarjuna</creator><creator>Vemula, Sateesh Kumar</creator><creator>Narala, Sagar</creator><creator>Munnangi, Sivaram</creator><creator>Repka, Michael A.</creator><general>Springer International Publishing</general><scope>C6C</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0009-0000-0848-8379</orcidid></search><sort><creationdate>20241217</creationdate><title>Formulation, Development, and Characterization of AMB-Based Subcutaneous Implants using PCL and PLGA via Hot-Melt Extrusion</title><author>Chitnis, Kshitij ; Narala, Nagarjuna ; Vemula, Sateesh Kumar ; Narala, Sagar ; Munnangi, Sivaram ; Repka, Michael A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c272t-30f4fa68c97a42010ca0bca896a9fd5ef168575908a0701dfe135428cf3817b93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Amlodipine - administration & dosage</topic><topic>Amlodipine - chemistry</topic><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Calorimetry, Differential Scanning - methods</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Delayed-Action Preparations - chemistry</topic><topic>Drug Compounding - methods</topic><topic>Drug Implants - chemistry</topic><topic>Drug Liberation</topic><topic>Drug Stability</topic><topic>Excipients - chemistry</topic><topic>Hot Melt Extrusion Technology - methods</topic><topic>Hot Temperature</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Polyesters - chemistry</topic><topic>Polylactic Acid-Polyglycolic Acid Copolymer - chemistry</topic><topic>Research Article</topic><topic>Solubility</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chitnis, Kshitij</creatorcontrib><creatorcontrib>Narala, Nagarjuna</creatorcontrib><creatorcontrib>Vemula, Sateesh Kumar</creatorcontrib><creatorcontrib>Narala, Sagar</creatorcontrib><creatorcontrib>Munnangi, Sivaram</creatorcontrib><creatorcontrib>Repka, Michael A.</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chitnis, Kshitij</au><au>Narala, Nagarjuna</au><au>Vemula, Sateesh Kumar</au><au>Narala, Sagar</au><au>Munnangi, Sivaram</au><au>Repka, Michael A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation, Development, and Characterization of AMB-Based Subcutaneous Implants using PCL and PLGA via Hot-Melt Extrusion</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2024-12-17</date><risdate>2024</risdate><volume>26</volume><issue>1</issue><spage>16</spage><pages>16-</pages><artnum>16</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>The hot-melt extrusion process is currently considered a prominent manufacturing technique in the pharmaceutical industry. The present study is intended to develop amlodipine besylate (AMB)-loaded subcutaneous implants to reduce the frequency of administration, thus improving patient compliance during hypertension management. AMB subcutaneous implants were prepared using continuous hot-melt extrusion technology using poly(caprolactone) and poly(lactic-co-glycolic acid) with dimensions of 3.70 cm (length) by 2.00 mm (diameter). The implants were characterized for thermal characteristics, drug-excipient incompatibilities, surface morphology, fracturability,
in vitro
drug release, and stability studies. Differential scanning calorimetry study confirmed the drug's crystalline state within the fabricated implants, while textural analysis demonstrated good fracturability in the lead formulation. Scanning electron microscopy revealed the smooth surface morphology of the lead subcutaneous implant. The lead formulation showed an extended drug release profile over 30 days (~ 2.25 mg per day) and followed zero-order release kinetics (R
2
value to 0.9999) with a mean dissolution time of 14.96 days. The lead formulation remained stable for 30 days at accelerated stability conditions of 40°C and 75% relative humidity. In conclusion, developing hot-melt extruded implants could be an alternative to the conventional amlodipine besylate (AMB) formulation.
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| subjects | Amlodipine - administration & dosage Amlodipine - chemistry Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology Calorimetry, Differential Scanning - methods Chemistry, Pharmaceutical - methods Delayed-Action Preparations - chemistry Drug Compounding - methods Drug Implants - chemistry Drug Liberation Drug Stability Excipients - chemistry Hot Melt Extrusion Technology - methods Hot Temperature Pharmacology/Toxicology Pharmacy Polyesters - chemistry Polylactic Acid-Polyglycolic Acid Copolymer - chemistry Research Article Solubility |
| title | Formulation, Development, and Characterization of AMB-Based Subcutaneous Implants using PCL and PLGA via Hot-Melt Extrusion |
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