Transdermal Iontophoresis of Insulin

Pillai, Omathanu; Panchagnula, Ramesh

doi:10.1159/000081114

Cited by 39 publications

(19 citation statements)

References 61 publications

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“…Moreover, both unsaturated fatty acids, oleic and linoleic acid produced permeation enhancement to the same extent for indomethacin [127] and arginine vasopressin [82], suggesting no effect of position and number of double bonds of unsaturated fatty acids on permeation enhancement. In contrast, increase in number of double bonds has been found to increase the permeation of some drugs like naloxone [128], alprazolam [129], paraaminobenzoic acid [47] and insulin [130]. In a recent study, the permeation of physostigmine ion paired with linoleic acid has been reported to be significantly lower than that ion paired with oleic acid.…”

Section: I) Fatty Acidsmentioning

confidence: 97%

Thermotropic and Spectroscopic Behavior of Skin: Relationship with Percutaneous Permeation Enhancement

Babita¹,

Kumar²,

Rana³

et al. 2006

CDD

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Stratum corneum (SC) is comprised of lipids, protein and low molecular weight water-soluble components. Changes in these skin micro constituents can be understood by instrumental methods like differential scanning calorimetry (DSC) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. The former provides information about changes in thermotropic behavior of SC lipids and proteins, whereas the latter provides data about alterations at molecular and conformational level. Most of the DSC thermograms of intact mammalian SC show two reversible and two irreversible transitions in the temperature range of 25-125 degrees C. The reversible endotherms are ascribed to lipid melting transitions, whereas the irreversible endotherms are ascribed to protein denaturation. Similarly, the FTIR spectral bands of SC occurring between 2920-2850 cm-1 and between 1650-1550 cm-1 have been suggested to arise from lipid and protein molecular vibrations, respectively. Treatment of skin with solvents or permeation enhancers alters the composition of lipids or their molecular arrangement in the skin microenvironment, which leads to changes in permeability of drug molecules. Furthermore, inhibition of lipid synthesis in epidermis with concomitant decrease in enthalpy of lipid endothermic transitions and reduction in height and area of asymmetric and symmetric C-H stretching peaks have been found to be directly correlated with enhanced permeation of drugs. In addition, method of skin preparation, type of skin, types of enhancer etc. also influence both the nature and intensity of responses recorded in spectrographs and thermograms. Therefore, the modification in spectrographs and thermograms of skin samples treated with various enhancers, vehicles etc. are expected to provide better insight into their mechanism of action on the skin. This review article shall critically evaluate the thermotropic and infrared spectroscopic data of SC/epidermis after various treatments.

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Section: I) Fatty Acidsmentioning

confidence: 97%

Thermotropic and Spectroscopic Behavior of Skin: Relationship with Percutaneous Permeation Enhancement

Babita¹,

Kumar²,

Rana³

et al. 2006

CDD

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“…This state of oxidative stress can result in injury to all the important cellular components like proteins, DNA and membrane lipids which can cause cell death. In recent years, increasing experimental and clinical data has provided compelling evidences for the involvement of oxidative stress in large number of pathological states including carcinogenesis [27]. Oxidative stress however, is not always detrimental but selective oxidative stress sometimes is desirable and can be utilized therapeutically also.…”

Section: Anticancer Activity Of Prepared Compoundsmentioning

confidence: 99%

Synthesis and anticancer effects of some novel pyrazolo[3,4-d]pyrimidine derivatives by generating reactive oxygen species in human breast adenocarcinoma cells

Rashad

Mahmoud

Ali

2011

European Journal of Medicinal Chemistry

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“…27,28) The absorption at 1740 cm Ϫ1 is from esterified carbonyl groups corresponding to endogenous skin lipids. 9) Figures 6a and b show the ATR-FTIR spectrum of rat skin treated with PBS solution (control) or 1.0% trypsin solution for 5 h. Compared with the control, some changes could be seen in the 1650 cm Ϫ1 region (amide I) and 1550 cm Ϫ1 region (amide II) in trypsin-treated skin samples (Fig. 6a).…”

Section: Atr-ftir Spectroscopymentioning

confidence: 99%

“…Most recent research has focused on the use of electrical energy to increase drug flux across the skin, including techniques such as iontophoresis, sonophoresis, electroporation, etc. [8][9][10] Unfortunately, the large, complex, and relatively uncharged insulin molecule still cannot across the intercellular lipid layer of the SC. The transport rate of hexameric insulin by iontophoresis across mouse skin has been low and variable.…”

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confidence: 99%

Transdermal Delivery of Insulin Using Trypsin as a Biochemical Enhancer

Quan

Zang

et al. 2008

Biological & Pharmaceutical Bulletin

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There are 30 million patients with diabetes mellitus worldwide, and 1.2 million new patients are diagnosed each year, including a growing number of children and young adults. 1)However, insulin has been administered only by parenteral routes for the therapeutic control of type 1 diabetes; many patients typically require injections of insulin a minimum of two to three times per day. To improve patient convenience and compliance, alternative routes have been investigated including nasal, oral, transdermal, buccal, ocular, rectal, and vaginal pathways. 2) Transdermal delivery of insulin can prevent its metabolization and the first-pass effect and may thus be an optimal route of administration. However, delivery of large molecules by the transdermal route is also limited by the unique bioarchitecture of skin, which has primarily evolved as a protective barrier against the entry of microorganisms and water.3)The stratum corneum (SC) barrier can be partially overcome by disruption of the lipid structure using fatty acids and surfactants as chemical penetration enhancers. [4][5][6] However, these enhancers are only useful for small molecules, 6,7) and it is difficult to achieve meaningful permeation of large peptides. Most recent research has focused on the use of electrical energy to increase drug flux across the skin, including techniques such as iontophoresis, sonophoresis, electroporation, etc. [8][9][10] Unfortunately, the large, complex, and relatively uncharged insulin molecule still cannot across the intercellular lipid layer of the SC. The transport rate of hexameric insulin by iontophoresis across mouse skin has been low and variable.11) Monomeric insulin analogues carrying two additional negative charges have demonstrated transport rates 50-100-fold higher than those of hexameric insulin. However, the quantity of delivery is still not sufficiently high to provide an effective basal insulin level (1 IU/h). 11)To overcome the barrier presented by the SC, proteolytic enzymes maybe used as skin penetration enhancers because their action is highly specific toward proteins and their molecular size is too large to permeate the viable epidermis. Such enzymes perhaps alter skin permeability by provoking biochemical and metabolic events within skin. For more than 50 years, proteolytic enzymes such as trypsin have been extensively used in laboratory settings for in vitro epidermal separation and keratinocyte isolation.12-15) The unique ability of proteases to cause selective epidermal separation has been in part explained by the proteolytic degradation of desmosomal proteins in the SC, which leads to cell dissociation. 16,17) Recently, several endogenous proteases occurring in the epidermis have been found to play important roles in regulating epidermal cell desquamation.18-21) Based on these findings, several therapeutic applications have been attempted for wound debridement and epidermal ablation. [22][23][24] However, no studies have examined the use of such proteolytic enzymes as a penetration enhancers for t...

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Transdermal Iontophoresis of Insulin

Cited by 39 publications

References 61 publications

Thermotropic and Spectroscopic Behavior of Skin: Relationship with Percutaneous Permeation Enhancement

Thermotropic and Spectroscopic Behavior of Skin: Relationship with Percutaneous Permeation Enhancement

Synthesis and anticancer effects of some novel pyrazolo[3,4-d]pyrimidine derivatives by generating reactive oxygen species in human breast adenocarcinoma cells

Transdermal Delivery of Insulin Using Trypsin as a Biochemical Enhancer

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