Assessment of simvastatin niosomes for pediatric transdermal drug delivery.
The prevalence of childhood dyslipidemia increases and is considered as an important risk factor for the incidence of cardiovascular disease in the adulthood. To improve dosing accuracy and facilitate the determination of dosing regimens in function of the body weight, the proposed study aims at preparing transdermal niosomal gels of simvastatin as possible transdermal drug delivery system for pediatric applications. Twelve formulations were prepared to screen the influence of formulation and processing variables on critical niosomal characteristics. Nano-sized niosomes with 0.31 μm number-weighted size displayed highest simvastatin release rate with 8.5% entrapment capacity. The niosomal surface coverage by negative charges was calculated according to Langmuir isotherm with n = 0.42 to suggest that the surface association was site-independent, probably producing surface rearrangements. Hypolipidemic activities after transdermal administration of niosomal gels to rats showed significant reduction in cholesterol and triglyceride levels while increasing plasma high-density lipoproteins concentration. Bioavailability estimation in rats revealed an augmentation in simvastatin bioavailability by 3.35 and 2.9 folds from formulation F3 and F10, respectively, compared with oral drug suspension. Hence, this transdermal simvastatin niosomes not only exhibited remarkable potential to enhance its bioavailability and hypolipidemic activity but also considered a promising pediatric antihyperlipidemic formulation.
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , KSA .|b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Zagazig University , Zagazig , Egypt .
Ahmed S
AS
Zidan
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , KSA .|c Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Beni Suef University , Beni Suef , Egypt , and.
Khaled M
KM
Hosny
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , KSA .|d Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Minia University , Minia , Egypt.
Osama A A
OA
Ahmed
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , King Abdulaziz University , Jeddah , KSA .
Usama A
UA
Fahmy
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D016503:Drug Delivery Systems; D050171:Dyslipidemias / Q000188:drug therapy* / Q000378:metabolism; D005782:Gels / Q000008:administration & dosage* / Q000737:chemistry; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D008075:Lipoproteins, HDL / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D019821:Simvastatin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D013535:Suspensions / Q000008:administration & dosage* / Q000737:chemistry
D005782:Gels; D000960:Hypolipidemic Agents; D008075:Lipoproteins, HDL; D008081:Liposomes; D013535:Suspensions; D019821:Simvastatin
Bioavailability; hypolipidemic activity; niosomes; simvastatin; transdermal delivery system