Derivatization of Steroids for Obtaining Conjugates: Use as Vectors for Drug Delivery

Faruk, Abdul; Ishar, M. P. S.

doi:10.18579/jpcrkc/2010/9/1/79469

Journal of Pharmaceutical Research

2010

DOI: 10.18579/jpcrkc/2010/9/1/79469

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Derivatization of Steroids for Obtaining Conjugates: Use as Vectors for Drug Delivery

Abdul Faruk¹,

M. P. S. Ishar²

Abstract: Mono-mode microwave assisted additions of-aminoacids (glycine / valine / phenylalanine) in the presence of K 2 CO 3 to 16 , 17-epoxy-3-hydroxypregnenolone (20) afford corresponding 17?-hydroxy-16-N-carboxyalkylaminosteroids (21a-c) in good yield. Similar conjugate addition of aminoacids to 16-dehydropregnenolone-3-acetate (15), under identical conditions, affords 16-N-carboxyalkylamino steroidal derivatives (22a-c). All the products have been purified chromatographically and characterized spectroscopically. Th… Show more

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Cited by 11 publications

References 14 publications

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In Vivo Testing and Extended Drug Release of Chitosan-Coated Itraconazole Loaded Microemulsion Using Volatile Oil Thymus vulgaris

Ebenazer

Franklyne

Tiwari

et al. 2020

Rev. Bras. Farmacogn.

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Microemulsions are potent drug delivery vehicles as they solubilize water insoluble drugs with poor bioavailability. The main aim of this study was to develop, optimize, and assess a thyme oil microemulsion with inherent antifungal activity for transdermal drug delivery of itraconazole. The optimized thyme oil microemulsion contains thyme oil, Cremophor EL, and water at 5:25:70% v/v respectively. The drug loaded microemulsion was mixed in equal proportion with chitosan for cutaneous application. The droplet size, zeta potential, FTIR spectra, and antifungal activity of the drug free microemulsion and drug loaded microemulsions with/without chitosan were characterized. The ex vivo drug permeation of drug loaded microemulsions with/without chitosan was compared with that of the bulk drug, using the Franz diffusion apparatus with the excised skin from Wistar rats. The droplet size of the drug free microemulsion and drug loaded microemulsions with/without chitosan were 25.53 ± 3.84 nm, 168.6 ± 13.33 nm, and 35.13 ± 0.41 nm respectively, with a polydispersity index between 0.436 and 0.658. The FTIR spectra demonstrated no changes in the structure of the drug in the drug loaded microemulsions with/without chitosan. The in vitro antifungal studies against Candida albicans exhibited similar zones of inhibition between bulk drug and drug loaded microemulsion, while the minimum inhibitory concentration showed a 2-fold decrease with drug loaded microemulsions with/without chitosan compared with the bulk drug. SEM confirmed substantial morphological changes in C. albicans cell membrane. The drug loaded microemulsion with chitosan revealed a slow and sustained release of itraconazole in phosphate buffered saline (pH 7.4) proving it to be an efficient, stable, and sustained topical delivery vehicle.

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In Vivo Testing and Extended Drug Release of Chitosan-Coated Itraconazole Loaded Microemulsion Using Volatile Oil Thymus vulgaris

Ebenazer

Franklyne

Tiwari

et al. 2020

Rev. Bras. Farmacogn.

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Design and development of an in situ synthesized layered double hydroxide structure of Fe-induced hydroxyapatite for drug carriers

et al. 2016

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Microemulsion loaded hydrogel as a promising vehicle for dermal delivery of the antifungal sertaconazole: design, optimization and ex vivo evaluation

Radwan

ElMeshad

Shoukri

2017

Drug Development and Industrial Pharmacy

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The purpose of the present study was to develop and optimize sertaconazole microemulsion-loaded hydrogel (STZ ME G) to enhance the dermal delivery and skin retention of the drug. Following screening of various oils for maximum drug solubility, 12 pseudoternary phase diagrams were constructed using oils (Peceol, Capryol 90), surfactants (Tween 80, Cremophor EL), a cosurfactant (Transcutol P) and water. A 2 × 3 × 2 × 3 full factorial design was employed to optimize a ME of desirable characteristics. The MEs were formulated by varying the oil type, oil concentration, surfactant type and surfactant: cosurfactant ratio. Optimized ME formulae F22 [5% Peceol, 55% Tween 80: Transcutol (1:2), 40% water] and F31 [5% Peceol, 55% Cremophor EL: Transcutol (1:2), 40% water] acquired mean droplet size of 75.21 and 8.68 nm, and zeta potential of 34.65 and 24.05 mV, respectively. Since F22 showed higher STZ skin retention during ex vivo studies (686.47 μg/cm) than F31 (338.11 μg/cm); hence it was incorporated in 0.5% Carbopol 934 gel to augment STZ skin retention capability. STZ ME G exhibited higher STZ skin retention (1086.1 μg/cm) than the marketed product "Dermofix cream" (270.3 μg/cm). The antimycotic activity against C.albicans revealed increased zones of inhibition for F22 and STZ ME G (35.75 and 30.5 mm, respectively) compared to Dermofix cream (26 mm). No histopathological changes were observed following topical application of STZ ME G on rats' skin (n = 9). Overall, the obtained results confirmed that the fabricated formulation could be a promising vehicle for the dermal delivery of STZ.

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Derivatization of Steroids for Obtaining Conjugates: Use as Vectors for Drug Delivery

Cited by 11 publications

References 14 publications

In Vivo Testing and Extended Drug Release of Chitosan-Coated Itraconazole Loaded Microemulsion Using Volatile Oil Thymus vulgaris

In Vivo Testing and Extended Drug Release of Chitosan-Coated Itraconazole Loaded Microemulsion Using Volatile Oil Thymus vulgaris

Design and development of an in situ synthesized layered double hydroxide structure of Fe-induced hydroxyapatite for drug carriers

Microemulsion loaded hydrogel as a promising vehicle for dermal delivery of the antifungal sertaconazole: design, optimization and ex vivo evaluation

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