Solid dispersion of lumefantrine using soluplus® by solvent evaporation method: formulation, characterization and in-vitro antimalarial screening
By: Kanojiya, Pranita Sunil
.
Contributor(s): Charde, Yogita.
Publisher: karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(1), Jan-Mar.Description: 121-132p.Subject(s): PHARMACOLOGYOnline resources: Click here
In:
Indian journal of pharmaceutical education and researchSummary: Objectives: Lumefantrine (LUM) is an antimalarial drug having poor aqueous solubility.
The objective was to formulate the solid dispersion of LUM and improve the solubility
and dissolution rate. Materials and Methods: Solvent evaporation technique was used
to prepare solid dispersions (SDs) with Soluplus® (SOL) using a rotary evaporator. The
feasibility of the formation of SD for LUM and SOL was assessed by the Hansen solubility
parameter. The drug solubility was analyzed by the HPLC method and the ratio of LUM:
SOL was optimized to 1:2. The SD was characterized by DSC, FTIR, XRD and SEM.
Results: The results showed that the LUM and SOL had groups that lead to the interaction
between them and this led to conversion from crystalline to amorphous form and thus
improved the dissolution rate. The solubility of L2 was found to be 135 ± 3.3 μg/mL
using the selected dissolution media (0.1 N HCl+1% Myrj 52). The
in-vitro antimalarial
screening was performed using the
P. falciparum 3D7 strain and the
in-vitro cytotoxicity
test was performed using the Vero cell line. The higher antimalarial efficacy of L2 SD
was observed as compared to plain LUM. The selectivity index value of LUM SD depicted
its non-toxicity. Stability study was carried out for three months and the SDs were
evaluated for the drug content, change in weight and
in-vitro drug release. No significant
changes were observed after three months in the drug content, SD weight and
in-vitro
drug release. Thus the L2 SD was found to be stable. Conclusion: The prepared SD
improved the solubility as well as the dissolution rate of the drug.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2022-1707 |
Objectives: Lumefantrine (LUM) is an antimalarial drug having poor aqueous solubility.
The objective was to formulate the solid dispersion of LUM and improve the solubility
and dissolution rate. Materials and Methods: Solvent evaporation technique was used
to prepare solid dispersions (SDs) with Soluplus® (SOL) using a rotary evaporator. The
feasibility of the formation of SD for LUM and SOL was assessed by the Hansen solubility
parameter. The drug solubility was analyzed by the HPLC method and the ratio of LUM:
SOL was optimized to 1:2. The SD was characterized by DSC, FTIR, XRD and SEM.
Results: The results showed that the LUM and SOL had groups that lead to the interaction
between them and this led to conversion from crystalline to amorphous form and thus
improved the dissolution rate. The solubility of L2 was found to be 135 ± 3.3 μg/mL
using the selected dissolution media (0.1 N HCl+1% Myrj 52). The
in-vitro antimalarial
screening was performed using the
P. falciparum 3D7 strain and the
in-vitro cytotoxicity
test was performed using the Vero cell line. The higher antimalarial efficacy of L2 SD
was observed as compared to plain LUM. The selectivity index value of LUM SD depicted
its non-toxicity. Stability study was carried out for three months and the SDs were
evaluated for the drug content, change in weight and
in-vitro drug release. No significant
changes were observed after three months in the drug content, SD weight and
in-vitro
drug release. Thus the L2 SD was found to be stable. Conclusion: The prepared SD
improved the solubility as well as the dissolution rate of the drug.
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