MUMBAI, India, July 13 -- Intellectual Property India has published a patent application (202641081627 A) filed by M. Mohan Varma; Dr. P. Shailaja; Mrs. Adilakshmi Challa; and Dr. S. Ramu on July 02, 2026, for Pharmaceutical Composition Containing Efavirenz Drug As Solid Lipid Nanoparticles For Intra Nasal ,nose To Brain Delivery.
Inventors include M. Mohan Varma; Dr. P. Shailaja; Mrs. Adilakshmi Challa; and Dr. S. Ramu.
The application for the patent was published on July 10, 2026, under issue no. 28/2026.
Abstract: ABSTRACT The present invention provides a novel intranasal pharmaceutical composition comprising efavirenz (EFV)-loaded solid lipid nanoparticles (SLNs) incorporated into a thermosensitive in-situ gel for enhanced nose-to-brain delivery. This system addresses the challenges of poor oral bioavailability, limited central nervous system (CNS) penetration, and first-pass metabolism associated with conventional EFV formulations. The optimized SLNs exhibit a mean particle size of approximately 108.5 nm, a polydispersity index (PDI) of 0.172, a zeta potential of -21.2 mV, and an entrapment efficiency of 64.9%. These nanoparticles are embedded in a poloxamer-based gel (poloxamer 188:407 in a 1:2 ratio) supplemented with 0.4% w/v Carbopol 934P as a mucoadhesive agent. The gel remains free-flowing at room temperature and undergoes rapid thermoreversible gelation at around 34°C within less than one minute, aligning perfectly with nasal mucosal conditions. In-vivo studies in Wistar rats demonstrated a remarkable brain-to-plasma ratio of 12.61% compared to 0.104% for oral administration, representing approximately a 120-fold enhancement in brain targeting, alongside an 80-fold increase in relative bioavailability. The formulation maintains long-term stability for 12 months under ICH conditions. This composition offers a safe, effective, and patient-friendly approach for targeting CNS HIV reservoirs while improving systemic absorption.
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