Limits...
Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy.

Ali MS, Alam MS, Alam N, Siddiqui MR - Iran J Pharm Res (2014)

Bottom Line: It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period.The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature.These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, K.S.A.

ABSTRACT
Benign prostatic hyperplasia (BPH)is the most common condition in aging men, associated with lower urinary tract symptoms. It is caused due to the augmented levels of the androgen dihydrotestosterone. Dutasteride, a 5α-Reductase inhibitor has been recommended for the treatment of BPH upon oral administration. However, long term oral administration of dutasteride may cause sexual problem in man. Therefore the main objective of this study was to develop transdermal patch having nanoemulsion gel of dutasteride in order to enhance physical and chemical stability and eliminate adverse effect of dutasteride. Optimized nanoemulsion was prepared by aqueous phase-titration method and characterized by droplet size, viscosity and refractive index. In-vitro skin permeation of dutasteride through rat abdominal skin was determined by the Franz diffusion cell.Significant increase in the steady state flux (J ss), permeability coefficient (K p) and enhancement ratio (E r) was observed in optimized nanoemulsion formulation A1 (p < 0.05). The Er of optimized nanoemulsion A1 was found to be 1.52 times with respect to control which indicates transdermal delivery may be better approach for BPH. Stability studies were performed for the period of 3 months. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p ≥ 0.05). The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature. These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation.

No MeSH data available.


Related in: MedlinePlus

Solubility of dutasteride in different oils at 25 °C (mean ± SD, n = 3).
© Copyright Policy
Related In: Results  -  Collection

License
getmorefigures.php?uid=PMC4232777&req=5

Figure 1: Solubility of dutasteride in different oils at 25 °C (mean ± SD, n = 3).

Mentions: Figure 1 depicts the solubility of dutasteride in different oils. The solubility of dutasteride was found to be highest in eucalyptus oil: oleic acid (1.5:1) 40.24 ± 1.56 mg/mL as compared to other oils. This may be attributed to the polarity of the poorly soluble drugs that favors their solubilization in small/medium molar volume of oils, such as medium-chain triglycerides or mono- or diglycerides. Oleic acid is used as penetration enhancer as well as medium for drug dissolving (19). Eucalyptus oil also act as medium for drug solubilization as well as penetration enhancer and is frequently used as an oil phase in steroidal drug (20). Low drug solubility would require incorporation of more oil to incorporate the target drug dose, which in turn would require higher surfactant concentration to achieve oil solubilization, which might increase the toxicity of the system. Thus, eucalyptus oil: oleic acid (1.5:1) was selected as the oil phase for the development of nanoemulsion formulation.


Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy.

Ali MS, Alam MS, Alam N, Siddiqui MR - Iran J Pharm Res (2014)

Solubility of dutasteride in different oils at 25 °C (mean ± SD, n = 3).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4232777&req=5

Figure 1: Solubility of dutasteride in different oils at 25 °C (mean ± SD, n = 3).
Mentions: Figure 1 depicts the solubility of dutasteride in different oils. The solubility of dutasteride was found to be highest in eucalyptus oil: oleic acid (1.5:1) 40.24 ± 1.56 mg/mL as compared to other oils. This may be attributed to the polarity of the poorly soluble drugs that favors their solubilization in small/medium molar volume of oils, such as medium-chain triglycerides or mono- or diglycerides. Oleic acid is used as penetration enhancer as well as medium for drug dissolving (19). Eucalyptus oil also act as medium for drug solubilization as well as penetration enhancer and is frequently used as an oil phase in steroidal drug (20). Low drug solubility would require incorporation of more oil to incorporate the target drug dose, which in turn would require higher surfactant concentration to achieve oil solubilization, which might increase the toxicity of the system. Thus, eucalyptus oil: oleic acid (1.5:1) was selected as the oil phase for the development of nanoemulsion formulation.

Bottom Line: It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period.The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature.These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, K.S.A.

ABSTRACT
Benign prostatic hyperplasia (BPH)is the most common condition in aging men, associated with lower urinary tract symptoms. It is caused due to the augmented levels of the androgen dihydrotestosterone. Dutasteride, a 5α-Reductase inhibitor has been recommended for the treatment of BPH upon oral administration. However, long term oral administration of dutasteride may cause sexual problem in man. Therefore the main objective of this study was to develop transdermal patch having nanoemulsion gel of dutasteride in order to enhance physical and chemical stability and eliminate adverse effect of dutasteride. Optimized nanoemulsion was prepared by aqueous phase-titration method and characterized by droplet size, viscosity and refractive index. In-vitro skin permeation of dutasteride through rat abdominal skin was determined by the Franz diffusion cell.Significant increase in the steady state flux (J ss), permeability coefficient (K p) and enhancement ratio (E r) was observed in optimized nanoemulsion formulation A1 (p < 0.05). The Er of optimized nanoemulsion A1 was found to be 1.52 times with respect to control which indicates transdermal delivery may be better approach for BPH. Stability studies were performed for the period of 3 months. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p ≥ 0.05). The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature. These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation.

No MeSH data available.


Related in: MedlinePlus