Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4þ and 16 þ ) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p50.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8 þ charge derived from four terminal arginines and MW of &1000 Da) showed greatest values for flux, Q 48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.

The present study reveals the successful application of sonophoresis in enhancing the permeation of peptide dendrimers across human skin.

The purpose of this investigation was to develop a ketoconazole cream with rosin for both topical and systemic delivery. Creams were prepared by using rosin as one of the components in different proportions with different cream base combinations. The drug excipients interaction studies were carried out and results revealed that there is no interaction between the drug and the excipients used in the formulation. The prepared creams were evaluated for their physicochemical properties, pH, viscosity, particle size, drug content and in vitro release studies. The release of the drug, ketoconazole was measured for eight hours and compared with a standard marketed formulation. The formulation (F8) fulfilled all topical formulation parameters; it can be used for the systemic topical drug delivery.

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