MyMedR

Cubosomes and hexosomes as versatile platforms for drug delivery

Azmi ID, Moghimi SM, Yaghmur A

Ther Deliv, 2015 Dec;6(12):1347-64.

Nonlamellar liquid crystalline phases are attractive platforms for drug solubilization and targeted delivery. The attractiveness of this formulation principle is linked to the nanostructural versatility, compatiblity, digestiblity and bioadhesive properties of their lipid constituents, and the capability of solubilizing and sustaining the release of amphiphilic, hydrophobic and hydrophilic drugs. Nonlamellar liquid crystalline phases offer two distinct promising strategies in the development of drug delivery systems. These comprise formation of ISAsomes (internally self-assembled 'somes' or particles) such as cubosomes and hexosomes, and in situ formation of parenteral dosage forms with tunable nanostructures at the site of administration. This review outlines the unique features of cubosomes and hexosomes and their potential utilization as promising platforms for drug delivery.

Intranasal nanoparticulate delivery systems for neurodegenerative disorders: a review

Babu SR, Shekara HH, Sahoo AK, Harsha Vardhan PV, Thiruppathi N, Venkatesh MP

Ther Deliv, 2023 Sep;14(9):571-594.

PMID: 37691577 DOI: 10.4155/tde-2023-0019

Neurodegenerative diseases are a significant cause of mortality worldwide, and the blood-brain barrier (BBB) poses a significant challenge for drug delivery. An intranasal route is a prominent approach among the various methods to bypass the BBB. There are different pathways involved in intranasal drug delivery. The drawbacks of this method include mucociliary clearance, enzymatic degradation and poor drug permeation. Novel nanoformulations and intranasal drug-delivery devices offer promising solutions to overcome these challenges. Nanoformulations include polymeric nanoparticles, lipid-based nanoparticles, microspheres, liposomes and noisomes. Additionally, intranasal devices could be utilized to enhance drug-delivery efficacy. Therefore, intranasal drug-delivery systems show potential for treating neurodegenerative diseases through trigeminal or olfactory pathways, which can significantly improve patient outcomes.

Fulltext Azelaic acid and Melaleuca alternifolia essential oil co-loaded vesicular carrier for combinational therapy of acne

Bisht A, Hemrajani C, Upadhyay N, Nidhi P, Rolta R, Rathore C, et al.

Ther Deliv, 2022 Jan;13(1):13-29.

PMID: 34842461 DOI: 10.4155/tde-2021-0059

Aim: Azelaic acid (AzA), a comedolytic, antibacterial, anti-inflammatory anti-melanogenic agent, prescribed against acne vulgaris is safe on skin. Its combination with another widely used anti-acne agent, tea tree oil (EO) whose delivery is limited by volatility, instability and lipophilicity constraints was attempted. Method: Solvent injection was used to prepare AzA-EO integrated ethosomes. Result: Ethosomes were transformed into carbopol hydrogel, which exhibited pseudo-plastic properties with appreciable firmness, work of shear, stickiness and work of adhesion. The hydrogel showed better permeation and retention characteristics vis-a-vis commercial formulation (AzidermTM), when evaluated in Wistar rat skin. Further, ethosome hydrogel composite was better tolerated with no side effects. Conclusion: The findings suggests that the aforementioned strategy could be a potential treatment used for acne management.

Solubility enhancement effect at absorption site on bioavailability of ritonavir using liquisolid technique

Bonthagarala B, Dasari V, Kotra V

Ther Deliv, 2019 May 01;10(5):295-310.

PMID: 31094300 DOI: 10.4155/tde-2019-0020

Aim: The present study revolved around determining the effect of increase in the solubility of these drugs at the absorption site using ritonavir as a drug model. Materials & methods: Ritonavir per-oral tablets were prepared using versatile and nonionic surfactants having high solubilization rate, which were further marked with high rate of dissolution. The high rate of dissolution formula applied to the solid state characterization by means of transition electron microscopy, differential scanning calorimetry, scanning electron microscopy, X-ray diffraction and infrared spectroscopy. Results & conclusion: The drug bioavailability was seen to increase expressively by administration of liquisolid tablets as compared with conventional tablets.

Nanomedicines for cancer therapy: current status, challenges and future prospects

Bor G, Mat Azmi ID, Yaghmur A

Ther Deliv, 2019 02;10(2):113-132.

PMID: 30678550 DOI: 10.4155/tde-2018-0062

The emergence of nanomedicine as an innovative and promising alternative technology shows many advantages over conventional cancer therapies and provides new opportunities for early detection, improved treatment, and diagnosis of cancer. Despite the cancer nanomedicines' capability of delivering chemotherapeutic agents while providing lower systemic toxicity, it is paramount to consider the cancer complexity and dynamics for bridging the translational bench-to-bedside gap. It is important to conduct appropriate investigations for exploiting the tumor microenvironment, and achieving a more comprehensive understanding of the fundamental biological processes in cancer and their roles in modulating nanoparticle-protein interactions, blood circulation, and tumor penetration. This review provides an overview of the current cancer nanomedicines, the major challenges, and the future opportunities in this research area.

Formulation and characterization of glibenclamide and quercetin-loaded chitosan nanogels targeting skin permeation

Chellappan DK, Yee NJ, Kaur Ambar Jeet Singh BJ, Panneerselvam J, Madheswaran T, Chellian J, et al.

Ther Deliv, 2019 May 01;10(5):281-293.

PMID: 31094299 DOI: 10.4155/tde-2019-0019

Aim: Our aim was to develop and characterize a nanogel formulation containing both glibenclamide and quercetin and to explore the permeation profile of this combination. Methods: Drug-loaded nanogel was prepared by ionic gelation. In addition, optimum encapsulation efficiencies of glibenclamide and quercetin were also obtained. The average nanoparticle size at optimum conditions was determined by Zetasizer. Results: The particle size of the nanogel was found to be 370.4 ± 4.78 nm with a polydispersity index of 0.528 ± 0.04, while the λ potential was positive in a range of 17.6 to 24.8 mV. The percentage cumulative drug release also showed favorable findings. Conclusion: The chitosan nanogel could be a potential alternative for delivering glibenclamide and quercetin through skin.

Thermoresponsive curcumin/DsiRNA nanoparticle gels for the treatment of diabetic wounds: synthesis and drug release

Katas H, Wen CY, Siddique MI, Hussain Z, Mohd Fadhil FH

Ther Deliv, 2017 01;8(3):137-150.

PMID: 28145827 DOI: 10.4155/tde-2016-0075

AIM: Chitosan (CS) has been extensively studied as drug delivery systems for wound healing. Results/methodology: CS nanoparticles were loaded with curcumin (Cur) and DsiRNA against prostaglandin transporter gene and they were incorporated into 20 and 25% w/v Pluronic F-127. The gels were later analyzed for their rheology, gelation temperature (Tgel), morphology, drug incorporation and in vitro drug release. The particle size was in the range of 231 ± 17-320 ± 20 nm, depending on CS concentration. The gels had Tgel of 23-28°C and exhibited sustained drug release with high accumulated amount of drugs over 48 h.

CONCLUSION: A thermo-sensitive gel containing Cur/DsiRNA CS nanoparticles was successfully developed and has a great potential to be further developed.

Nano-drug delivery system: a promising approach against breast cancer

Malik JA, Ansari JA, Ahmed S, Khan A, Ahemad N, Anwar S

Ther Deliv, 2023 May;14(5):357-381.

PMID: 37431741 DOI: 10.4155/tde-2023-0020

Breast cancer (BC) is among the most frequent malignancies women face around the globe. Nanotherapeutics are constantly evolving to overcome the limitations of conventional diagnostic and therapeutic approaches. Nanotechnology-based nanocarriers have a higher entrapment efficiency, low cytotoxicity, greater stability and improved half-life than conventional therapy. Nano-drug delivery systems have improved pharmacokinetics and pharmacodynamics parameters because of nanomeric size. Currently, various nano-formulations are in preclinical and clinical settings for breast cancer, like polymeric nanoparticles, micelles, nanobodies, magnetic nanoparticles, liposomes, niosomes, gold-nanoparticles, dendrimers and carbon-nanotubes. This review highlights the recent advancement in developing nano-drug delivery systems for BC treatment. This review will open the gateway to researchers to understand the current approaches to developing nano-formulation and improving problems associated with conventional therapy.

Fulltext Gastric ulcer healing by chebulinic acid solid dispersion-loaded gastroretentive raft systems: preclinical evidence

Negi P, Gautam S, Sharma A, Rathore C, Sharma L, Upadhyay N, et al.

Ther Deliv, 2022 Feb;13(2):81-93.

PMID: 35075915 DOI: 10.4155/tde-2021-0062

Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.

Fulltext An overview of vaccine development for COVID-19

Shahcheraghi SH, Ayatollahi J, Aljabali AA, Shastri MD, Shukla SD, Chellappan DK, et al.

Ther Deliv, 2021 03;12(3):235-244.

PMID: 33624533 DOI: 10.4155/tde-2020-0129

The COVID-19 pandemic continues to endanger world health and the economy. The causative SARS-CoV-2 coronavirus has a unique replication system. The end point of the COVID-19 pandemic is either herd immunity or widespread availability of an effective vaccine. Multiple candidate vaccines - peptide, virus-like particle, viral vectors (replicating and nonreplicating), nucleic acids (DNA or RNA), live attenuated virus, recombinant designed proteins and inactivated virus - are presently under various stages of expansion, and a small number of vaccine candidates have progressed into clinical phases. At the time of writing, three major pharmaceutical companies, namely Pfizer and Moderna, have their vaccines under mass production and administered to the public. This review aims to investigate the most critical vaccines developed for COVID-19 to date.

Fulltext Can Amphotericin B-mediated effects be limited using intranasal versus intravenous route?

Siddiqui R, Yee Ong TY, Maciver S, Khan NA

Ther Deliv, 2023 Aug;14(8):485-490.

PMID: 37691579 DOI: 10.4155/tde-2023-0032

Aim: CNS infections due to parasites often prove fatal. In part, this is due to inefficacy of drugs to cross the blood-brain barrier. Methods: Here, we tested intranasal and intravenous route and compared adverse effects of Amphotericin B administration, through blood biochemistry, liver, kidney and brain histopathological evidence of toxicities in vivo post-administration. Results: It was observed that intranasal route limits the adverse side effects of Amphotericin B, in contrast to intravenous route. Conclusion: As parasites such as Naegleria fowleri exhibit unequivocal affinity toward the olfactory bulb and frontal lobe in the central nervous system, intranasal administration would directly reach amoebae bypassing the blood-brain barrier selectivity and achieve the minimum inhibitory concentration at the target site.

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