<p>The Siddha herb Nilavembu (<i>Andrographis paniculata</i>) is a potent traditional remedy known for its anti-inflammatory, antipyretic, and antiviral properties. It is a highly valued traditional medicine for respiratory illness both in Siddha and Ayurvedic medicine. Recent studies have revealed that the active ingredient, andrographolide, inhibits the replication of dengue virus serotype 1(DENV1) and chikungunya virus. The antiviral potential of Nilavembu Kudineer (NVK) has also been highlighted in studies, making it a promising candidate for managing viral infections. Orodispersible films (ODFs) are thin polymeric films which dissolve rapidly in the oral cavity, providing ease of administration. This study hypothesizes that formulating Nilavembu as an ODF would improve patient compliance and enhance the delivery of its bioactive compounds. In this study, Nilavembu ODFs were formulated, characterized, and evaluated for antimicrobial activity against broad range of microorganisms confirming their antimicrobial activity against resistant isolates. The MIC values were expressed with bactericidal activity observed from 70&#xa0;µg/mL and complete inhibition at 100&#xa0;µg/mL. Antioxidant assays revealed strong radical scavenging activity (up to nearly 85% at 120&#xa0;µg/mL). The cytotoxicity assay was conducted to assess the viability of the extract in VERO cells, producing no significant reduction in viability. The films displayed rapid disintegration (&lt; 1&#xa0;min), acceptable thickness (0.2&#xa0;mm), and folding endurance of 28 folds, exceeding the standard benchmarks for stability. In-vitro dissolution studies were performed to evaluate the drug release of Nilavembu ethanolic extract capsules in phosphate buffer (pH 6.8). The test formulation exhibited higher cumulative release compared to the control capsule. These findings indicated improved dissolution characteristics of the formulated capsule proving enhanced bioavailabiity. Molecular docking demonstrated potent inhibitory interactions of andrographolide derivatives with SARS-CoV-2 proteins, with binding affinities of -6.49&#xa0;kcal/mol for 3CLpro, -8.357&#xa0;kcal/mol for RdRp, and − 5.572&#xa0;kcal/mol for spike, validated against remdesivir as a control ligand. Further, In- silico pharmacokinetic evaluation was done for the bioactive compounds in Nilavembu reporting it as non-hepatotoxic, non-carcinogenic and non-mutagenic, where Andrographolide showed favourable ADMET properties. These findings suggested that Nilavembu ODF is a promising drug delivery system.</p>

错误:搜索内容不能为空,请输入英文关键词
错误:关键词超出字数限制,请精简
高级检索

Nilavembu Orodispersible Film as a Drug Delivery System – a Novel Approach

  • Mohamed Abdus Salam,
  • Susan Silvia N,
  • Mahalakshmi Velrajan

摘要

The Siddha herb Nilavembu (Andrographis paniculata) is a potent traditional remedy known for its anti-inflammatory, antipyretic, and antiviral properties. It is a highly valued traditional medicine for respiratory illness both in Siddha and Ayurvedic medicine. Recent studies have revealed that the active ingredient, andrographolide, inhibits the replication of dengue virus serotype 1(DENV1) and chikungunya virus. The antiviral potential of Nilavembu Kudineer (NVK) has also been highlighted in studies, making it a promising candidate for managing viral infections. Orodispersible films (ODFs) are thin polymeric films which dissolve rapidly in the oral cavity, providing ease of administration. This study hypothesizes that formulating Nilavembu as an ODF would improve patient compliance and enhance the delivery of its bioactive compounds. In this study, Nilavembu ODFs were formulated, characterized, and evaluated for antimicrobial activity against broad range of microorganisms confirming their antimicrobial activity against resistant isolates. The MIC values were expressed with bactericidal activity observed from 70 µg/mL and complete inhibition at 100 µg/mL. Antioxidant assays revealed strong radical scavenging activity (up to nearly 85% at 120 µg/mL). The cytotoxicity assay was conducted to assess the viability of the extract in VERO cells, producing no significant reduction in viability. The films displayed rapid disintegration (< 1 min), acceptable thickness (0.2 mm), and folding endurance of 28 folds, exceeding the standard benchmarks for stability. In-vitro dissolution studies were performed to evaluate the drug release of Nilavembu ethanolic extract capsules in phosphate buffer (pH 6.8). The test formulation exhibited higher cumulative release compared to the control capsule. These findings indicated improved dissolution characteristics of the formulated capsule proving enhanced bioavailabiity. Molecular docking demonstrated potent inhibitory interactions of andrographolide derivatives with SARS-CoV-2 proteins, with binding affinities of -6.49 kcal/mol for 3CLpro, -8.357 kcal/mol for RdRp, and − 5.572 kcal/mol for spike, validated against remdesivir as a control ligand. Further, In- silico pharmacokinetic evaluation was done for the bioactive compounds in Nilavembu reporting it as non-hepatotoxic, non-carcinogenic and non-mutagenic, where Andrographolide showed favourable ADMET properties. These findings suggested that Nilavembu ODF is a promising drug delivery system.