Development of non-invasive transdermal patch of Emblica officinalis for anti atherosclerotic activity

The present study was designed to formulate matrix type transdermal patches of a potent anti atherosclerotic botanical Emblica officinalis on a mercury substrate and evaluated for physicochemical parameters like thickness, % flatness, weight variation, moisture uptake, moisture content, folding endurance, elongation and drug content values. Further, in vivo drug release was also observed by HPLC in rabbit serum. Four formulations were prepared using different ratio of matrix forming polymers, plasticizer and penetration enhancers. Formulations E-1, E-2, E-3 and E-4 were composed of Ethyl cellulose (EC) and Hydroxypropyl Methylcellulose (HPMC) with the following ratios: 6:4, 7:3, 8:2 and 9:1. In vitro cumulative amounts of the permeated drug were observed 48.53, 55.46, 73.26 and 99.72% in 48 hrs from the four formulations. The release profile of the optimized formulation E-4; r2 = 0.984 (Higuchi) showed that permeation of the drug controlled by a diffusion mechanism. The cumulative amount of the permeated drug after 48hrs from E-4 was 343.95mcg/cm2. Permeability coefficient was calculated 7.16mcg/cm2/hr. Based on physicochemical and in vitro skin permeation studies, E-4 was chosen for further in vivo studies. Blood plasma concentration of E-4 after 48 hrs was 0.2914mcg/cm2. Skin permeation performance and scanning electron microscopic studies revealed that formulation E-4 was found to be better than other formulations and it was selected as the optimized formulation. The skin irritation tests showed negligible erythema and edema. The developed transdermal patches may increase the efficacy of E. officinalis for the therapy of atherosclerosis

Development of non-invasive transdermal patch of Emblica officinalis for anti atherosclerotic activity

The present study was designed to formulate matrix type transdermal patches of a potent anti atherosclerotic botanical Emblica officinalis on a mercury substrate and evaluated for physicochemical parameters like thickness, % flatness, weight variation, moisture uptake, moisture content, folding endurance, elongation and drug content values. Further, in vivo drug release was also observed by HPLC in rabbit serum. Four formulations were prepared using different ratio of matrix forming polymers, plasticizer and penetration enhancers. Formulations E-1, E-2, E-3 and E-4 were composed of Ethyl cellulose (EC) and Hydroxypropyl Methylcellulose (HPMC) with the following ratios: 6:4, 7:3, 8:2 and 9:1. In vitro cumulative amounts of the permeated drug were observed 48.53, 55.46, 73.26 and 99.72% in 48 hrs from the four formulations. The release profile of the optimized formulation E-4; r2 = 0.984 (Higuchi) showed that permeation of the drug controlled by a diffusion mechanism. The cumulative amount of the permeated drug after 48hrs from E-4 was 343.95mcg/cm2. Permeability coefficient was calculated 7.16mcg/cm2/hr. Based on physicochemical and in vitro skin permeation studies, E-4 was chosen for further in vivo studies. Blood plasma concentration of E-4 after 48 hrs was 0.2914mcg/cm2. Skin permeation performance and scanning electron microscopic studies revealed that formulation E-4 was found to be better than other formulations and it was selected as the optimized formulation. The skin irritation tests showed negligible erythema and edema. The developed transdermal patches may increase the efficacy of E. officinalis for the therapy of atherosclerosis

Hg²⁺ induced hydrolysis of pentaquinone based Schiff base: A new chemodosimeter for Hg²⁺ ions in mixed aqueous media

A pentaquinone based compound 3 has been synthesized which works as a selective and sensitive chemodosimeter for mercury ions via Hg²⁺ promoted hydrolysis of an imine linkage to generate a fluorescent change in mixed aqueous media

New fluorogenic sensors for Hg²⁺ ions: Through-bond energy transfer from pentaquinone to rhodamine

New pentaquinone derivatives 5 and 8 having rhodamine moieties have been designed and synthesized that undergo through-bond energy transfer (TBET) in the presence of Hg2+ ions among the various cations (Cu2+, Pb2+, Fe2+, Fe3+, Zn2+, Ni2+, Cd2+, Co2+, Ag+, Ba2+, Mg2+, K+, Na+, and Li+) tested in mixed aqueous media

Recognition of adenosine monophosphate and H₂PO₄^– using zinc ensemble of new hexaphenylbenzene derivative: Potential bioprobe and multichannel keypad system

Zinc ensemble of hexaphenylbenzene derivative 3 exhibits sensitive response toward adenosine monophosphate (AMP) and H2PO4– ions. Further, the application of derivative 3 as a multichannel molecular keypad could be realized in the presence of inputs of Zn2+ ions, H2PO4– ions, and AMP

Highly selective fluorescence turn-on chemodosimeter based on rhodamine for nanomolar detection of copper ions

A highly selective fluorescent chemodosimeter based on rhodamine is synthesized which undergoes Cu2+ driven hydrolysis in aqueous media to produce fluorescence turn-on changes with a detection limit up to the nanomolar range

A charge transfer assisted fluorescent probe for selective detection of hydrogen peroxide among different reactive oxygen species

A charge transfer assisted fluorescent probe is synthesized which undergoes a change in fluorescence emission at two different wavelengths in the presence of hydrogen peroxide

Thiacalix[4]arene based fluorescent probe for sensing and imaging of Fe³⁺ ions

A thiacalix[4]arene based fluorescent chemosensor 3 in the cone conformation has been synthesized and its recognition behaviour is evaluated toward various metal ions in mixed aqueous media. The chemosensor 3 showed high selectivity towards Fe3+ ions by fluorescence quenching of excimer emission. Further, evaluation of the 3· Fe3+ complex prepared in situ demonstrated great promise for the detection of the Fe3+ ion in the presence of amino acids, blood serum and bovine serum albumin (BSA) solution. The compound 3 has suitable permeability into the PC3 cells and can be utilized as a Fe3+ selective sensor in living cells (PC3 cells)

Naphthalimide appended rhodamine derivative: Through bond energy transfer for sensing of Hg²⁺ions

A naphthalimide appended rhodamine based fluorescent chemosensor ‘1’ is synthesized which undergoes through bond energy transfer in the presence of Hg2+ ions in mixed aqueous media