Title:Formulation Development and Assessment of Solid Dispersion and
Hydrotropy for BCS Class II Drug Solubility Enhancement
Volume: 21
Issue: 2
Author(s): Neha Bajwa, Mela Singh, Srishti Naryal, Shipra Mahal, Sumit Mehta, Jitender Madan and Ashish Baldi*
Affiliation:
- Pharma Innovation Lab, Department of Pharmaceutical Sciences & Technology, Maharaja Ranjit Singh Punjab Technical University, Bathinda-151001, Punjab, India
Keywords:
Bioavailability, cyclodextrin, dissolution, hydrotropy, permeability, solid dispersion.
Abstract:
Aim: This study aimed to evaluate the potential of different hydrophilic polymers to increase
Arteether's water solubility.
Background: Arteether is classified as a class II biopharmaceutical in the Biopharmaceutical Classification
System (BCS), with low water solubility (17 g/mL) and dissolution rate, resulting in poor bioavailability.
Objective: The goal of this research is to improve the water solubility of Arteether (ART) by using a solid
dispersion and hydrotropic approach with a variety of carriers, such as PEG-6000 PVP K-30, Poloxamer-
188, Poloxamer-407, HPMC E 15LV, HPMC K-100M, sucrose, and mannitol, sodium benzoate, sodium
citrate, Urea, nicotinamide, and beta-cyclodextrin.
Methods: Melting and evaporation methods were used to make the solid dispersion. Instrumental examinations,
including XRD, DSC, FTIR, and SEM, confirmed any physical changes caused by the interaction
of ART and carriers.
Results: The most significant increase in water solubility of Arteether was discovered with CD:
PEG600:Pol -407, and the highest enhancement in solubility was 67 times. While 37.34 times and 49
times increase in solubility was observed at 1:4.3:3.7 weight ratio of AE: PEG-6000:Poloxamer-407 40
percent mix of nicotinamide, respectively. The in vitro results show that ART's dissolution rate in the
solid dispersion system was dramatically reduced compared to pure drug. This might be because of the
drug's enhanced wettability, dispersion ability, and transition from crystalline to amorphous form. Compared
to the ART itself, the permeability of Arteether from solid dispersion was increased up to 7 times.
However, the permeability of solid cyclodextrin dispersion was extremely low, just 4.42 times. This may
be due to the drug encapsulation in the cyclodextrin cavity.
Conclusion: This research successfully developed and optimized various polymer and solubility enhancement
approaches for Arteether, resulting in increased water solubility, which may improve Arteether's
oral bioavailability. The findings of this study might be utilized to develop an oral dosage of
Arteether with enhanced bioavailability.
