FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF TRANSDERMAL DRUG DELIVERY SYSTEMS CONTAINING EPLERENONE

Objective: The proposed work was aimed at optimization, formulation, and characterization of transdermal patches of eplerenone for efficient transdermal delivery of the drug. Methods: The log p estimation of eplerenone is 1.34, it was closer to standard worth. Log P value in a range of 1 to 4 indicates higher permeation through the skin. FTIIR study was carried out individually for drug, each polymer, and finished product (Patches) compared eplerenone and FTIR spectra of pure drug and polymer. The calibration curve of eplerenone in Phosphate buffer pH 6.8 was analyzed. Results: The selected range of eplerenone was found to be linear. A regression coefficient (R2) at 245 nm was found to be 0.994. Drug content outcomes additionally discovered uniform in all clusters in a range of 97 % to 98 %, that batches arranged with ERS 100 show great mechanical properties contrast with different polymers however helpless glue properties. The flatness of 4 cm2 patches ranges from 348±0.087 mg to 387±0.527 mg. skin irritation it was produced irritation with negligible erythema following 10 d and unequivocal erythema, promptly obvious edema was produced following 12 d. Conclusion: These after-effects of the in vivo skin irritation study recommended that advanced batch S9 doesn't show any kind of significant disturbance on rodent skin for as long as 14 d and it was securely utilized around 24 h. the optimized batch S9 drug was constantly discharged through the Wistar rodent skin up to 16 hr and the delivery design was like an in vitro dissolution profile of the market product.

Nanoemulsion-based dissolving microneedle arrays for enhanced intradermal and transdermal delivery

The development of dissolving microneedles (DMN) is one of the advanced technologies in transdermal drug delivery systems, which precisely deliver the drugs through a rapid dissolution of polymers after insertion into the skin. In this study, we fabricated nanoemulsion-loaded dissolving microneedle (DMN) arrays for intradermal and transdermal drug delivery. For this task, model drug (amphotericin B, AmB)-loaded nanoemulsion (NE) were prepared by the probe-sonication method. AmB-loaded-NE was prepared using Capmul MCM C-8 EP/NF, Tween® 80, poly(vinyl alcohol) (PVA-10 kDa), and poly (vinyl pyrrolidone) (PVP-360 kDa or K29/32) by using SpeedMixer™, followed by probe-sonication and evaluated for particle size and polydispersity index (PDI). Transmission electron microscopy (TEM) was also used to assess the particle size before and after DMN casting. AmB-NE embedded DMN arrays were found to be strong enough, revealed efficient skin insertion, and penetrated down to the fourth layer (depth ≈ 508 μm) of Parafilm M® (validated skin model). Ex vivo skin deposition experiments in full-thickness neonatal porcine demonstrated that after 24 h, AmB-NE-DMN arrays were able to deposit 111.05 ± 48.4 µg/patch AmB into the skin. At the same time, transdermal porcine skin permeation studies showed significantly higher permeability of AmB (29.60 ± 8.23 μg/patch) from AmB-NE-DMN compared to MN-free AmB-NE patches (5.0 ± 6.15 μg/patch) over 24 h. Antifungal studies of optimized AmB-NE-DMN, AmB-loaded discs and drug-free DMN against Candida albicans, confirmed the synergistic activity of Campul-MCM C-8, used in the nanoemulsion formulation. This study establishes that nanoemulsion based dissolving microneedle may serve as an efficient system for intradermal as well as transdermal drug delivery. Graphical abstract

Application of Gas Chromatography for the Analysis of Residual Solvents in Transdermal Drug Delivery Systems (TDS)

Background: Transdermal drug delivery systems (TDS) are widely used to deliver a number of different drug therapeutics. The design delivery can be impacted by excipients and, more broadly, organic solvents. Organic or residual solvents are routinely monitored due to safety concerns. However, there is little information on the mechanical properties and delivery performance of TDS. Objective: The objective of this study was to develop and validate an efficient GC-Headspace method to determine the residual solvents (n-heptane, o-xylene, and ethyl acetate) in transdermal patches. The analytical method was applied to monitor residual solvents in TDS and evaluate the potential effect of the residual solvent levels on the TDS adhesion properties. Methods: An Agilent GC 7890A was integrated with an Agilent headspace analyzer 7697A system and was used for method development, analytical method validation, and the testing phases of the study. For the analysis of residual solvents in TDS, 2cm x 3cm, a TDS sample was placed in a 20 mL Headspace vial containing 2 mL of a DMSO/water (1:1, v/v) solvent mixture, and an external standard (cyclohexane) was extracted by the headspace analyzer. The system suitability test was conducted according to USP <621>, and analytical method validation was conducted according to USP <1225> over 3 days for validation and was also performed during in-study sample analysis. Results: The resolution between the solvents was acceptable (2.5, %RSD = 8.0). Intra- and inter-day accuracy and precision of all quality control standards as well as the spiked standards in the transdermal patches were found to be acceptable with RSD% ≤ 10% and accuracy ≥ 85%, respectively. Linearity was > 0.99 for all analytes. Conclusion: The validated GC-Headspace method was successfully applied to a pilot study for in-house manufactured TDS patches to study the impact of residual solvent concentration on adhesion performance.

Transdermal Drug delivery: A step towards treatment of cancer

Background: Transdermal drug delivery is an emerging and tempting system over oral and hypodermic drug delivery system. With the new developments in skin penetration techniques, anticancer drugs ranging from hydrophilic macromolecules to lipophilic drugs can be administered via transdermal route to treat cancer. Objective: In the present review, various approaches to enhance the transdermal delivery of drugs is discussed including the micro and nanotechnology based transdermal formulations like chemotherapy, gene therapy, immunotherapy, phototherapy, vaccines and medical devices. Limitations and advantages of various transdermal technologies is also elaborated. Method: In this review, patent applications and recent literature of transdermal drug delivery systems employed to cure mainly cancer are covered. Results: Transdermal drug delivery systems have proved their potential to cure cancer. They increase the bioavailability of drug by site specific drug delivery and can reduce the side effects/toxicity associated with anticancer drugs. Conclusion: The potential of transdermal drug delivery systems to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

Transdermal Drug Delivery Systems and Their Use in Obesity Treatment

Transdermal drug delivery (TDD) has recently emerged as an effective alternative to oral and injection administration because of its less invasiveness, low rejection rate, and excellent ease of administration. TDD has made an important contribution to medical practice such as diabetes, hemorrhoids, arthritis, migraine, and schizophrenia treatment, but has yet to fully achieve its potential in the treatment of obesity. Obesity has reached epidemic proportions globally and posed a significant threat to human health. Various approaches, including oral and injection administration have widely been used in clinical setting for obesity treatment. However, these traditional options remain ineffective and inconvenient, and carry risks of adverse effects. Therefore, alternative and advanced drug delivery strategies with higher efficacy and less toxicity such as TDD are urgently required for obesity treatment. This review summarizes current TDD technology, and the main anti-obesity drug delivery system. This review also provides insights into various anti-obesity drugs under study with a focus on the recent developments of TDD system for enhanced anti-obesity drug delivery. Although most of presented studies stay in animal stage, the application of TDD in anti-obesity drugs would have a significant impact on bringing safe and effective therapies to obese patients in the future.

Electrospun Nanofiber and Cryogel of Polyvinyl Alcohol Transdermal Patch Containing Diclofenac Sodium: Preparation, Characterization and In Vitro Release Studies

Transdermal drug delivery systems (TDDS) have drawn more interest from pharmaceutical scientists because they could provide steady blood levels and prevent the first-pass metabolism over a longer period. Polyvinyl alcohol (PVA) has been widely used in this application due to its biocompatibility, non-toxicity, nanofiber and hydrogel-forming ability. Despite those benefits, their morphology would easily be destroyed by continuous water absorption and contribute to burst drug release due to its hydrophilicity. The aim of this study was to prepare the diclofenac sodium (DS)-medicated dual layer PVA patch using a combination of electrospinning and cryogelation (freeze–thaw) methods to improve the physicochemical properties and drug compatibility and investigate the release of the DS-medicated dual layer PVA patch. Morphological observations using scanning electron microscopy (SEM) verified the polymer−polymer interaction between both layers, whereas Fourier transform infrared (FTIR) spectroscopy has demonstrated the compatibility of DS in PVA matrix up to 2% w/v of PVA volume. The DS loads were found amorphously distributed efficaciously in PVA matrix as no visible spectra of DS–PVA interaction were detected. The DS-medicated dual layer PVA patch with a thicker nanofiber layer (3-milliliter running volume), three freeze–thaw cycles and 2% DS loading labeled as 2%DLB3C show the lowest swelling capacity (18.47%). The in vitro assessment using Franz diffusion cells showed that the 2%DLB3C indicates a better sustained release of DS, with 53.26% of the DS being released after 12 h. The 2%DLB3C owned a flux (Jss) of 0.256 mg/cm2/h and a permeability coefficient (Kp) value of 0.020 cm/h. Thus, the results demonstrate that DS-medicated dual layer PVA patches prepared via a combination of electrospinning and cryogelation are capable of releasing drugs for up to 24 h and can serve as a drug reservoir in the skin, thereby extending the pharmacologic effects of DS.

Green Fabrication and Release Mechanisms of pH-Sensitive Chitosan–Ibuprofen Aerogels for Controlled Transdermal Delivery of Ibuprofen

Ibuprofen is a potent non-steroidal anti-inflammatory drug due to its analgesic, antipyretic, and anti-inflammatory actions. However, its poor solubility in water makes it difficult to manufacture ibuprofen tablets, which limited the application of ibuprofen in drug delivery systems. Polymer–drug aerogels have attracted huge interest in optimizing the drug delivery efficiency and improving the physicochemical characteristics and therapeutic quality. Here, chitosan–ibuprofen aerogels with excellent swelling, high biocompatibility, and better drug delivery efficiency were synthesized by a simple method. Our study found that the chitosan–ibuprofen aerogels exhibited remarkably improved thermal stability, excellent swelling ratio, and high drug loading. As a consequence of these favorable properties, the chitosan–ibuprofen aerogels exhibited improved drug delivery efficiency and achieved drug prolonged administration. Our study highlights the great potential of polymer–drug aerogels in improving the drug delivery efficiency of transdermal drug delivery systems.

Review on Transferosomes and Transferosomal Gels

Transdermal drug delivery systems (TDDS), which are self-administrable and non-invasive, can improve bioavailability and patient compliance by bypassing first-pass metabolism. Vesicular-based TDDS have attracted a lot of attention in recent years because they're designed for controlled, efficient, and targeted drug delivery. One of these delivery technologies, transferosomal-based formulations, has grown in popularity due to its ability to achieve all of the desired criteria and quality qualities. Transferosomes combine the characteristics of liposomes and niosomes because they contain both liposomes (phospholipids and cholesterols) and niosomes as components (nonionic surfactants; edge activators). as a result, they are referred to as the first generation of elastic liposomes. However transdermal drug delivery is difficult due to the presence of the skin's protective barrier, transferosomal drug delivery overcomes all obstacles due to its unique characteristics, such as its ultradeformable vesicular nature. The benefits, limitations, modes of penetration, formulations, production and assessment methodologies, and pharmaceutical uses of transferosomal drug delivery systems are discussed in this paper. Conclusion: Transferosomes have several importance over other vesicular systems, including greater deformability, greater penetration power across skin, the ability to deliver systemic drugs, and higher stability.