Preformulation Studies and Pseudo-Ternary Phase Diagram Development for Dolutegravir Sodium: A Foundational Step toward SMEDDS Design

Indian Journal of Pharmaceutical Education and Research

  • Jayadev Hiremath1Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagara, Karnataka, INDIA.
  • Nimbagal Raghavendra Naveen1Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagara, Karnataka, INDIA.
  • Prakash Goudanavar1Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagara, Karnataka, INDIA.
  • Girish Meravanige3Department of Biomedical Sciences, College of Medicine, King Faisal University, Al-Ahsa, Al-Ahsa, SAUDI ARABIA .
  • Santosh Fattepur4School of Pharmacy, Management and Science University, Seksyen 13, Shah Alam, Selangor, MALAYSIA.
  • Rashed M. Almuqbil5Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Al-Ahsa, SAUDI ARABIA.
  • Bandar Aldhubiab5Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Al-Ahsa, SAUDI ARABIA.
  • Sreeharsha Nagaraja5Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Al-Ahsa, SAUDI ARABIA.

Volume 59 Issue 3s Pages s874-s880

DOI: 10.5530/ijper.20252845

Abstract

Background: Dolutegravir Sodium (DTG) is a poorly soluble antiretroviral drug that will find it difficult to achieve oral bioavailability. Preformulation and screening of excipients are mandatory as a stepping stone in formulation development. Objectives: To conduct comprehensive preformulation studies and build pseudo-ternary phase diagrams for DTG with a view to informing future development of a stable SMEDDS formulation. Materials and Methods: UV spectrophotometry was used to establish the maxima of absorption and to construct a standard calibration curve for DTG. Solubility studies were performed using various oils and surface-active agents. The efficiency of emulsification was used to screen the surfactants, while compatibility was established through the use of FTIR spectroscopy. Pseudo-ternary diagrams identified microemulsion regions with Capmul MCM C8 oil and Kolliphor EL/propylene glycol Smix. Results: Enhanced solubility of DTG has been observed in Capmul MCM C8. Kolliphor EL and propylene glycol were chosen to be the surfactant and co-surfactant, respectively, for their emulsification capacity and high transmittance (>94%). FTIR established no meaningful incompatibilities between DTG and chosen excipients. Of Smix ratios examined, 3:1 (Kolliphor EL:PG) showed the largest microemulsion area in pseudo-ternary phase diagrams. Conclusion: The study offers a clear preformulation platform for DTG, determining important excipients and a best-fit Smix ratio for microemulsion development. Ternary phase diagrams were constructed to confirm the choice of ingredients for a possible SMEDDS. Subsequent research will construct on this basis to develop and assess a DTG-loaded SMEDDS for enhanced oral bioavailability

Keywords

  • Dolutegravir sodium
  • Ternary Phase Diagram
  • SMEDDS
  • Lipid Based Systems
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