Essential oils enriched self-nano-emulsifying systems for effective oral delivery of zaleplon for improvement of insomnia treatment
By: El-Enin, Hadel A. Abo
.
Contributor(s): Khalifa, Amany Salah.
Publisher: Bangalore Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(4), Oct-Dec.Description: 1031-1043p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical education and researchSummary: Background: Insomnia is usually associated with mental and physical daytime
impairment. Zaleplon (Zp) is indicated in insomnia management but its limited aqueous
solubility led to its low bioavailability (BAV) ~30%. Self-nanoemulsifying drug delivery
system (SNEDDS) was a recommended nano-delivery system for improvement poorly
soluble drugs’ oral bioavailability. Consequently, this study aimed to prepare SNEDDS
entrapped Zp using essential oils (EOs) have insomnia management effect. Materials
and Methods: Different EOs, surfactants and co-surfactants in varying ratios were used
in preparing Zp-loaded SNEDDS, which were chosen according to their ability to ease
the emulsification and improve Zp solubility. To optimize the formulations; Zp-SNEEDS
formulae were characterized for particle-size, zeta-potential, emulsification-time, and
drug loading capacity. Additionally,
in-vitro release and stability studies were performed
to provide a perception on the stability and enhancing Zp release from Zp-SNEDDS
formulae. To improve Zp-SNEDDS activity; BAV study and psychomotor evaluation test
were carried out in albino mice. Results: The selected optimized formulae containing
Tween80, PEG400 and anise oil had nanoparticle size (~98nm), loading capacity up
to 40%, emulsification time~34sec and increased Zp dissolution rate up to 2 folds
compared to pure Zp suspension. Zp-SNEEDS’ BAV is 1.29 and increases in the sleep
time up to 165min which equal to the synergetic effect of anise oil and zaleplon alone.
Conclusion: The significant increase in the rate and extent of Zp oral absorption from
nano-positively charge Zp-SNEEDS with high BAV and increases in sleeping time indicates
the effectiveness of Zp-SNEEDS in improving Zp oral absorption and therapeutic effect
in insomnia treatment.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2023-0100 |
Background: Insomnia is usually associated with mental and physical daytime
impairment. Zaleplon (Zp) is indicated in insomnia management but its limited aqueous
solubility led to its low bioavailability (BAV) ~30%. Self-nanoemulsifying drug delivery
system (SNEDDS) was a recommended nano-delivery system for improvement poorly
soluble drugs’ oral bioavailability. Consequently, this study aimed to prepare SNEDDS
entrapped Zp using essential oils (EOs) have insomnia management effect. Materials
and Methods: Different EOs, surfactants and co-surfactants in varying ratios were used
in preparing Zp-loaded SNEDDS, which were chosen according to their ability to ease
the emulsification and improve Zp solubility. To optimize the formulations; Zp-SNEEDS
formulae were characterized for particle-size, zeta-potential, emulsification-time, and
drug loading capacity. Additionally,
in-vitro release and stability studies were performed
to provide a perception on the stability and enhancing Zp release from Zp-SNEDDS
formulae. To improve Zp-SNEDDS activity; BAV study and psychomotor evaluation test
were carried out in albino mice. Results: The selected optimized formulae containing
Tween80, PEG400 and anise oil had nanoparticle size (~98nm), loading capacity up
to 40%, emulsification time~34sec and increased Zp dissolution rate up to 2 folds
compared to pure Zp suspension. Zp-SNEEDS’ BAV is 1.29 and increases in the sleep
time up to 165min which equal to the synergetic effect of anise oil and zaleplon alone.
Conclusion: The significant increase in the rate and extent of Zp oral absorption from
nano-positively charge Zp-SNEEDS with high BAV and increases in sleeping time indicates
the effectiveness of Zp-SNEEDS in improving Zp oral absorption and therapeutic effect
in insomnia treatment.
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