Development and Optimization of <i>Andrographis paniculata</i> Extract-Loaded Self-Microemulsifying Drug Delivery System Using Experimental Design Model

• Main Authors: Chaiyakarn Pornpitchanarong (Author), Prasert Akkaramongkolporn (Author), Nattawat Nattapulwat (Author), Praneet Opanasopit (Author), Prasopchai Patrojanasophon (Author)
• Format: Book
• Published: MDPI AG, 2024-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics16020166; 1999-4923
• Keywords: <i>Andrographis paniculata</i>; andrographolide; self-microemulsifying drug delivery system; experimental design; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 16, Iss 2, p 166 (2024)

The objectives of this study were to develop an optimized formulation for an <i>Andrographis paniculata</i> extract (AGPE)-loaded self-microemulsifying drug delivery system (SMEDDS) using an experimental design and evaluate the characteristics of the developed SMEDDS. The solubility of andrographolide (AGP) in various solvents was investigated. The pseudo-ternary phase was constructed to provide an optimal range for each component to form microemulsions (MEs). The formulation was optimized using an I-optimal design mixture type, where the physical stability, droplet size, polydispersity index, and zeta potential were examined. Soft capsules of the optimized AGPE-loaded SMEDDS were manufactured. The dissolution and ex vivo membrane permeation were studied. Oleic acid, Tween^® 80, and PEG 400 were the best solubilizers for AGP. The promising surfactant to co-surfactant ratio to generate ME was 3:1. The optimized SMEDDS contained 68.998% Tween^® 80, with 13.257% oleic acid and 17.745% PEG 400. The assayed content of AGP, uniformity of dosage unit, and stability complied with the expected specifications. The dissolution and membrane permeability of AGPE-loaded SMEDDS was significantly improved from the <i>A. paniculata</i> extract (<i>p</i> < 0.05). All in all, the developed optimized AGPE-loaded SMEDDS was proven to contain optimal composition and AGP content where a stable ME could spontaneously be formed with enhanced delivery efficacy.