Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride

He, Jingjing; Zhang, Zichen; Zheng, Xianzi; Li, Lü; Qi, Jianping; Wu, Wei; Lü, Yi

doi:10.3390/pharmaceutics13040579

Cited by 46 publications

(31 citation statements)

References 75 publications

(29 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In this study, an aqueous blend of PVA and PVP was used in the DMN formulation with various concentrations, as shown in Table . Previous studies have shown that the combination of these two polymers results in better mechanical strength and penetration ability than when used singly. , PVP is a polymer with good hardness, but when used alone, it will provide inadequate mechanical strength for DMN due to its hygroscopicity. , The addition of PVA will fix the shortcomings of PVP. The combination of PVA and PVP causes the formation of hydrogen bonds between the CO group of PVP and the −OH group of PVA to provide adequate mechanical strength .…”

Section: Resultsmentioning

confidence: 99%

“…When applied, DMN will form small pores as channels for the drug or drug MPs to pass through . DMN-loaded drugs can deliver drugs directly; meanwhile, for drug MPs, it is necessary to pass through the polymer matrix first after being released from DMN . This causes the MPs in the DMN to permeate less than the pure drug in the same time duration and provides longer MTF availability.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Glucose-Responsive Microparticle-Loaded Dissolving Microneedles for Selective Delivery of Metformin: A Proof-of-Concept Study

et al. 2023

View full text Add to dashboard Cite

Diabetes mellitus (DM) is a metabolic disorder that is one of the most common health problems in the world, primarily type 2 DM (T2DM). Metformin (MTF), as the first-line treatment of DMT2, is effective in lowering glucose levels, but its oral administration causes problems, including gastrointestinal side effects, low bioavailability, and the risk of hypoglycemia. In this study, we formulated MTF into microparticles incorporating a glucose-responsive polymer (MP−MTF−GR), which could potentially increase the bioavailability and extend and control the release of MTF according to glucose levels. This system was delivered by dissolving microneedles (MP−MTF−GR−DMN), applied through the skin, thereby preventing gastrointestinal side effects of orally administered MTF. MP−MTF−GR was formulated using various concentrations of gelatin as a polymer combined with phenylboronic acid (PBA) as a glucose-responsive material. MP−MTF−GR was encapsulated in DMN using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA) as DMN polymers. The physicochemical evaluation of MP−MTF−GR showed that MTF could be completely entrapped in MP with the percentage of MTF trapped increasing with increasing gelatin concentration without changing the chemical structure of MTF and producing stable MP. In addition, the results of the physicochemical evaluation of MP−MTF−GR−DMN showed that DMN had adequate mechanical strength properties and penetration ability and was stable to environmental changes. The results of the in vitro release and ex vivo permeation study on media with various concentrations of glucose showed that the release and permeation of MTF from the formula increased with increasing glucose levels in the media. The MP−MTF−GR−DMN formula successfully delivered MTF through the skin at 11.30 ± 0.29, 23.31 ± 1.64, 36.12 ± 3.77, and 53.09 ± 3.01 μg from PBS, PBS + glucose 1%, PBS + glucose 2%, and PBS + glucose 4%, respectively, at 24 h, which indicates glucose-responsive permeation and release behavior. The formula developed was also proven to be nontoxic based on hemolysis tests. Importantly, the in vivo study on the rat model showed that this combination approach could provide a better glucose reduction compared to other routes, reducing the blood glucose level to normal levels after 3 h and maintaining this level for 8 h. Furthermore, this approach did not change the skin moisture of the rats. This MP−MTF−GR−DMN is a promising alternative to MTF delivery to overcome MTF problems and increase the effectiveness of T2DM therapy.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Glucose-Responsive Microparticle-Loaded Dissolving Microneedles for Selective Delivery of Metformin: A Proof-of-Concept Study

et al. 2023

View full text Add to dashboard Cite

show abstract

“…In a recent study, He et al . fabricated DMNs by a two-step casting procedure that used HA and PVP as matrix materials for loading propranolol hydrochloride in needle tips ( Figure 10 ) 158 . The MNs had outstanding mechanical strength to penetrate SC, as well as superior dissolution ability to release propranolol hydrochloride.…”

Section: The Applications Of Nanocarrier- or Mn-based Transdermal Del...mentioning

confidence: 99%

“…(C) Fluorescence microscopy images of the MNs with fluorescein isothiocyanate isomer (FITC) as a tracer reagent. Adapted with permission from reference 158 . Copyright 2021 Multidisciplinary Digital Publishing Institute.…”

Section: Figurementioning

confidence: 99%

Advanced nanocarrier- and microneedle-based transdermal drug delivery strategies for skin diseases treatment

Qu¹,

Geng²,

Liu³

et al. 2022

Theranostics

103

View full text Add to dashboard Cite

Skin diseases are the fourth leading cause of nonfatal and chronic skin diseases, acting as a global burden and affecting the world economy. Skin diseases severely impact the patients' quality of life and have influenced their physical and mental state. Treatment of these skin disorders with conventional methods shows a lack of therapeutic efficacy, long treatment duration, recurrence of the condition, and systemic side effects due to improper drug delivery. However, these pitfalls can be overcome with the applications of advanced nanocarrier- and microneedle (MN)-based transdermal drug delivery strategies that provide efficient site-specific drug delivery at the target site. These advanced transdermal drug delivery strategies can be more effective than other drug administration routes by avoiding first-pass metabolism, enhancing the drug concentration in local skin lesions, and reducing systemic toxicity. Compared with traditional transdermal delivery methods, nanocarrier- or MN-based drug delivery systems are painless, noninvasive, or minimum-invasive and require no expensive equipment. More importantly, they can introduce more advanced functions, including increased skin penetration efficiency, controlled drug release rates, enhanced targeting abilities, and theranostic functions. Here, the emergence of versatile advanced transdermal drug delivery systems for the transdermal delivery of various drugs is reviewed, focusing on the design principles, advantages, and considerations of nanocarrier- and MN-based transdermal drug delivery strategies and their applications in treating diverse skin diseases, including psoriasis, dermatitis, melanoma, and other skin diseases. Moreover, the prospects and challenges of advanced transdermal delivery strategies for treating dermatological disorders are summarized.

show abstract

“…Oral NSAIDs, such as ibuprofen sustained-release tablets and ibuprofen sustained-release capsules, are nonselective cyclooxygenase (COX) enzyme inhibitors, which can simultaneously inhibit COX-1 and COX-2 (Thakur et al., 2018 ). However, the inhibition of COX-1 could cause gastrointestinal discomfort (Solomon et al., 2017 ). The selective COX-2 inhibitor Celecoxib has low solubility (3–7 μg/ml), strong first-pass metabolism and rapid plasma clearance rate, so Celecoxib capsules have only 22–40% bioavailability when administered orally (Quinones & Pierre, 2019 ).…”

Section: Drug Dosage Form For Treating Ramentioning

confidence: 99%

Transdermal delivery of inflammatory factors regulated drugs for rheumatoid arthritis

et al. 2022

View full text Add to dashboard Cite

Rheumatoid arthritis is a chronic autoimmune disease, with the features of recurrent chronic inflammation of synovial tissue, destruction of cartilage, and bone erosion, which further affects joints tissue, organs, and systems, and eventually leads to irreversible joint deformities and body dysfunction. Therapeutic drugs for rheumatoid arthritis mainly reduce inflammation through regulating inflammatory factors. Transdermal administration is gradually being applied to the treatment of rheumatoid arthritis, which can allow the drug to overcome the skin stratum corneum barrier, reduce gastrointestinal side effects, and avoid the first-pass effect, thus improving bioavailability and relieving inflammation. This paper reviewed the latest research progress of transdermal drug delivery in the treatment of rheumatoid arthritis, and discussed in detail the dosage forms such as gel (microemulsion gel, nanoemulsion gel, nanomicelle gel, sanaplastic nano-vesiclegel, ethosomal gel, transfersomal gel, nanoparticles gel), patch, drug microneedles, nanostructured lipid carrier, transfersomes, lyotropic liquid crystal, and drug loaded electrospinning nanofibers, which provide inspiration for the rich dosage forms of transdermal drug delivery systems for rheumatoid arthritis.

show abstract

Design and Evaluation of Dissolving Microneedles for Enhanced Dermal Delivery of Propranolol Hydrochloride

Cited by 46 publications

References 75 publications

Glucose-Responsive Microparticle-Loaded Dissolving Microneedles for Selective Delivery of Metformin: A Proof-of-Concept Study

Glucose-Responsive Microparticle-Loaded Dissolving Microneedles for Selective Delivery of Metformin: A Proof-of-Concept Study

Advanced nanocarrier- and microneedle-based transdermal drug delivery strategies for skin diseases treatment

Transdermal delivery of inflammatory factors regulated drugs for rheumatoid arthritis

Contact Info

Product

Resources

About