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Pioglitazone solid dispersion system prepared by spray drying method: in vitro and in vivo evaluation
Varsha Pokharkar1, Manisha Kutwal, Leenata Mandpe
1Bharati Vidyapeeth University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune, Maharashtra, India.
PDA Journal of Pharmaceutical Science and Technology
|February 7, 2013
Summary
Spray drying created pioglitazone solid dispersions with improved solubility and dissolution. This enhanced pioglitazone
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Pioglitazone, a thiazolidinedione, improves insulin sensitivity but exhibits poor aqueous solubility and dissolution.
- Low solubility and dissolution limit the oral bioavailability and therapeutic efficacy of pioglitazone.
- Developing strategies to enhance pioglitazone's solubility is crucial for effective diabetes management.
Purpose of the Study:
- To improve the aqueous solubility and dissolution rate of pioglitazone using solid dispersion technology.
- To prepare pioglitazone solid dispersions via spray drying with hydrophilic polymers.
- To evaluate the impact of solid dispersion on the in vivo hypoglycaemic activity of pioglitazone.
Main Methods:
- Pioglitazone solid dispersions were prepared using spray drying with hydrophilic polymers (PVP K17, PVP K30, HPMC E3).
- Characterization involved solubility, particle size, surface area, DSC, FTIR, XRD, and in vitro dissolution testing.
- In vivo hypoglycaemic activity was assessed in Alloxan-induced diabetic Swiss Albino mice.
Main Results:
- Solid dispersions, particularly with PVP K17, showed significantly enhanced solubility and dissolution rates compared to pure pioglitazone.
- The optimized solid dispersion formulation demonstrated a two-fold increase in glucose inhibition compared to the pure drug.
- Spray-dried solid dispersions exhibited improved pharmacodynamic activity and antihyperglycemic effects in vivo.
Conclusions:
- Solid dispersion formulation via spray drying effectively enhances pioglitazone's aqueous solubility and dissolution.
- Improved in vitro properties translate to significantly enhanced in vivo hypoglycaemic activity.
- This approach offers a promising strategy for improving the therapeutic potential of poorly soluble drugs like pioglitazone.
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