Transdermal delivery of antidiabetic drugs: formulation and delivery strategies

Ahad, Abdul; Al-Saleh, Ahmad M.; Akhtar, Naseem; Al-Mohizea, Abdullah M.; Al-Jenoobi, Fahad I.

doi:10.1016/j.drudis.2015.06.002

Cited by 36 publications

(16 citation statements)

References 54 publications

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“…Nano-sized particles are capable to work as pharmaceutical carriers for various delivery system; orally, transdermally, or intravenously. Studies show that NPs have been tremendously used in the biomedical sector to treat diseases like diabetes [ 7 , 8 , 9 ] and cancer [ 10 , 11 , 12 ]. Additionally, particle size plays an important role in controlling the efficiency of transporting therapeutic agents by conventional ways.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Optimization of Chitosan Nanoparticles Loaded with L-Ascorbic Acid and Thymoquinone

et al. 2018

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The combination of compounds with different classes (hydrophobic and hydrophilic characters) in single chitosan carrier is a challenge due to the hydrophilicity of chitosan. Utilization of l-ascorbic acid (LAA) and thymoquinone (TQ) compounds as effective antioxidants is marred by poor bioavailability and uptake. Nanoparticles (NPs) solved the problem by functioning as a carrier for them because they have high surface areas for more efficient delivery and uptake by cells. This research, therefore, synthesized chitosan NPs (CNPs) containing LAA and TQ, CNP-LAA-TQ via ionic gelation routes as the preparation is non-toxic. They were characterized using electron microscopy, zetasizer, UV–VIS spectrophotometry, and infrared spectroscopy. The optimum CNP-LAA-TQ size produced was 141.5 ± 7.8 nm, with a polydispersity index (PDI) of 0.207 ± 0.013. The encapsulation efficiency of CNP-LAA-TQ was 22.8 ± 3.2% for LAA and 35.6 ± 3.6% for TQ. Combined hydrophilic LAA and hydrophobic TQ proved that a myriad of highly efficacious compounds with poor systemic uptake could be encapsulated together in NP systems to increase their pharmaceutical efficiency, indirectly contributing to the advancement of medical and pharmaceutical sectors.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Optimization of Chitosan Nanoparticles Loaded with L-Ascorbic Acid and Thymoquinone

et al. 2018

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“…The biggest challenge in the development of transdermal systems is to reduce the barrier property of skin without causing harm and local irritation to the skin. 3 , 4 …”

Section: Introductionmentioning

confidence: 99%

Formulation design and development of matrix diffusion controlled transdermal drug delivery of glimepiride

Akram¹,

Ahmad²,

Abrar³

et al. 2018

DDDT

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BackgroundThe present work was conducted to prepare and evaluate transdermal patches with optimization of suitable polymeric blend of poly(meth) acrylates (Eudragit®) (Ammonio Methacrylate Copolymer Ph Eur) for sustained transdermal delivery of glimepiride.MethodPolymeric matrix transdermal films were prepared by using Ammonio Methacrylate Copolymer Ph Eur RL 100 and Ammonio Methacrylate Copolymer Ph Eur RS 100 as the film former, and dibutyl phthalate (30% w/w) as the plasticizer. Patches were characterized by physical appearance, thickness, weight variation, folding endurance, percentage erosion, swelling index, moisture content, and moisture uptake capacity. Fourier transform infrared spectroscopic studies and differential scanning calorimetry analysis of physical mixtures of contents were performed to identify any chemical and physical interaction between drug and excipients. Five different enhancers (isopropyl myristate [IPM], Span® 80, Tween® 20, eucalyptus oil, and limonene) were employed at three different concentrations of polymer (2%, 5%, and 10% w/w) in order to enhance permeation through rabbit skin. In vitro drug release studies were performed at pH 7.4, and scanning electron microscopy was conducted to elucidate surface morphology before and after the drug release. In vitro permeation studies through rabbit skin were performed on Franz diffusion cells and permeation kinetics followed the Higuchi model.ResultsResults of in vitro permeation studies revealed that these enhancers not only increased drug release but also augmented the skin permeation of glimepiride.ConclusionIPM was the most effective enhancer with the highest permeation flux of 51.763 μg/cm2/hr, and the enhancement effect of different enhancers on glimepiride permeation through rabbit skin was in the rank order of IPM > eucalyptus oil > Span® 80 > Tween® 20> limonene.

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“…Transdermal drug delivery systems are designed so that the drug can be delivered at a predetermined and controlled rate (Ahad et al 2015b(Ahad et al , 2016, which is particularly conducive to treating chronic disorders like hypertension (Ahad et al 2013a). Correspondingly, the adverse effects and inconvenience concomitant with oral route are circumvented.…”

Section: Introductionmentioning

confidence: 99%

Invasomes of isradipine for enhanced transdermal delivery against hypertension: formulation, characterization, and in vivo pharmacodynamic study

Qadri

Ahad

Aqil

et al. 2016

Artificial Cells, Nanomedicine, and Biotechnology

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Context Isradipine is an effective calcium channel blocker used in the management of hypertension. It undergoes extensive first pass metabolism and has low oral bioavailability. Hence we attempted to develop isradipine-loaded invasomes. Objective The purpose of this work was to prepare and characterize invasomes carrier for isradipine, and to evaluate the optimized formulation obtained for pharmacodynamic study. Materials and methods Isradipine-loaded invasomes were prepared by conventional thin layer evaporation technique using Phospholipon® 90G, β-citronellene (terpene) and ethanol. Prepared formulations were characterized in terms of size, size distribution, morphology, entrapment efficiency, and antihypertensive activity. Results and discussion It was observed that prepared isradipine-loaded invasomes delivers ameliorated flux, reasonable entrapment efficiency, and more effectiveness for transdermal delivery. The optimized formulation presented the particle size of 194 ± 18 nm, entrapment efficiency (88.46%), and attained mean transdermal flux of 22.80 ± 2.10 μg/cm/h through rat skin. Confocal laser scanning microscopy revealed an enhanced permeation of Rhodamine-Red-loaded isradipine invasomes to the deeper layers of the rat skin. During antihypertensive study, the treatment group showed a substantial and constant decrease in blood pressure, for up to 24 h. The isradipine invasomes formulation was found to be effective, with a 20% reduction in blood pressure by virtue of better permeation through Wistar rat skin. Conclusion It was concluded that the developed isradipine invasomes accentuate the transdermal flux and the results obtained encouraged the use of the isradipine-loaded invasomes as the formulation for the potential management of hypertension.

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Transdermal delivery of antidiabetic drugs: formulation and delivery strategies

Cited by 36 publications

References 54 publications

Synthesis and Optimization of Chitosan Nanoparticles Loaded with L-Ascorbic Acid and Thymoquinone

Synthesis and Optimization of Chitosan Nanoparticles Loaded with L-Ascorbic Acid and Thymoquinone

Formulation design and development of matrix diffusion controlled transdermal drug delivery of glimepiride

Invasomes of isradipine for enhanced transdermal delivery against hypertension: formulation, characterization, and in vivo pharmacodynamic study

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