NERDG 2026
Poster 16 Abstract
Design of a Solid Supersaturated Self-Nanoemulsifying System: Role of Apinovex in Modulating Drug Precipitation
Kranthi Gattu, Akanksha Ravindra Ugale, Shashank Reddy Pasika
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Jamaica, NY 11439, USA
Presenting Author: Kranthi Gattu
Corresponding Author: Ketan Patel, [email protected]
Purpose
Supersaturated self-nanoemulsifying drug delivery systems are widely explored to enhance the dissolution of poorly water-soluble drugs; however, rapid drug recrystallization and incomplete drug release remain significant formulation challenges. The present study aimed to develop a solid supersaturated self-nanoemulsifying preconcentrate (S-superSNEP) of sorafenib, a model drug selected due to its poor aqueous solubility and BCS class II classification. Dimethylacetamide (DMA) was employed as a supersaturation solvent, while novel polymer Apinovex (APNX), a high-molecular-weight polyacrylic acid-based excipient, was explored as a precipitation inhibitor to stabilize supersaturation following aqueous dilution. In the present work, APNX was specifically explored for its role in modulating precipitation behavior and sustaining supersaturation in a solid SNEDDS platform.
Methods
Sorafenib-loaded supersaturated self-nanoemulsifying preconcentrates were prepared using DMA, medium-chain triglycerides, and Kolliphor® EL. Solidification was achieved using a co-processed excipient composed of microporous silica (Florite 100) and polyvinyl alcohol (PVA) in a 1:1 weight ratio, which had been previously optimized in our lab for both adsorption capacity and flow properties. APNX was incorporated at different concentrations to modulate precipitation behavior. Optimized formulations were characterized in terms of Globule size, Zeta potential, Precipitation Kinetics, and In-vitro dissolution under both sink and non-sink conditions.
Results
The optimized formulation containing 2% w/v sorafenib spontaneously formed nanoemulsions with a mean globule size of 56 ± 2.7 nm and a zeta potential of −7.19 ± 1.2 mV, indicating efficient self-nano emulsification. Precipitation studies conducted over 48 hours demonstrated rapid drug precipitation in aqueous media. In contrast, formulations containing APNX at different concentrations showed a reduction in precipitation, indicating concentration-dependent stabilization of supersaturation. These findings were further supported by qualitative and quantitative assessments, which confirmed suppression of crystalline growth in APNX containing systems. The solid S-superSNEP exhibited significantly faster and higher drug release compared to the plain sorafenib.
Conclusion
The combined use of DMA as a supersaturation solvent, APNX as a polymeric precipitation inhibitor, and a PVA–Florite® 100 based co-processed excipient enabled the successful development of a solid supersaturated SNEDDS of sorafenib, offering a promising strategy to mitigate precipitation-induced loss of supersaturation and enhance dissolution of poorly water-soluble drugs.
Keywords
Supersaturated SNEDDS; precipitation inhibition; Apinovex polymer; solid SNEDDS; dissolution enhancement
Poster 16 Abstract
Design of a Solid Supersaturated Self-Nanoemulsifying System: Role of Apinovex in Modulating Drug Precipitation
Kranthi Gattu, Akanksha Ravindra Ugale, Shashank Reddy Pasika
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Jamaica, NY 11439, USA
Presenting Author: Kranthi Gattu
Corresponding Author: Ketan Patel, [email protected]
Purpose
Supersaturated self-nanoemulsifying drug delivery systems are widely explored to enhance the dissolution of poorly water-soluble drugs; however, rapid drug recrystallization and incomplete drug release remain significant formulation challenges. The present study aimed to develop a solid supersaturated self-nanoemulsifying preconcentrate (S-superSNEP) of sorafenib, a model drug selected due to its poor aqueous solubility and BCS class II classification. Dimethylacetamide (DMA) was employed as a supersaturation solvent, while novel polymer Apinovex (APNX), a high-molecular-weight polyacrylic acid-based excipient, was explored as a precipitation inhibitor to stabilize supersaturation following aqueous dilution. In the present work, APNX was specifically explored for its role in modulating precipitation behavior and sustaining supersaturation in a solid SNEDDS platform.
Methods
Sorafenib-loaded supersaturated self-nanoemulsifying preconcentrates were prepared using DMA, medium-chain triglycerides, and Kolliphor® EL. Solidification was achieved using a co-processed excipient composed of microporous silica (Florite 100) and polyvinyl alcohol (PVA) in a 1:1 weight ratio, which had been previously optimized in our lab for both adsorption capacity and flow properties. APNX was incorporated at different concentrations to modulate precipitation behavior. Optimized formulations were characterized in terms of Globule size, Zeta potential, Precipitation Kinetics, and In-vitro dissolution under both sink and non-sink conditions.
Results
The optimized formulation containing 2% w/v sorafenib spontaneously formed nanoemulsions with a mean globule size of 56 ± 2.7 nm and a zeta potential of −7.19 ± 1.2 mV, indicating efficient self-nano emulsification. Precipitation studies conducted over 48 hours demonstrated rapid drug precipitation in aqueous media. In contrast, formulations containing APNX at different concentrations showed a reduction in precipitation, indicating concentration-dependent stabilization of supersaturation. These findings were further supported by qualitative and quantitative assessments, which confirmed suppression of crystalline growth in APNX containing systems. The solid S-superSNEP exhibited significantly faster and higher drug release compared to the plain sorafenib.
Conclusion
The combined use of DMA as a supersaturation solvent, APNX as a polymeric precipitation inhibitor, and a PVA–Florite® 100 based co-processed excipient enabled the successful development of a solid supersaturated SNEDDS of sorafenib, offering a promising strategy to mitigate precipitation-induced loss of supersaturation and enhance dissolution of poorly water-soluble drugs.
Keywords
Supersaturated SNEDDS; precipitation inhibition; Apinovex polymer; solid SNEDDS; dissolution enhancement
