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

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 579
Author(s):  
Jingjing He ◽  
Zichen Zhang ◽  
Xianzi Zheng ◽  
Lu Li ◽  
Jianping Qi ◽  
...  

Oral propranolol hydrochloride has been the first-line treatment for infantile hemangioma (IH), whereas systemic exposure to propranolol has the potential of causing serious adverse reactions. Dermal delivery of propranolol is preferable due to high local drug concentration and fewer adverse effects. However, propranolol hydrochloride (BCS class I) is highly hydrophilic and has difficulty in penetrating the stratum corneum (SC) barrier. Dissolving microneedles (MNs) are an efficient tool for overcoming the barrier of the SC and enhancing dermal drug delivery. In this study, propranolol hydrochloride-loaded dissolving MNs were fabricated by using hyaluronic acid and polyvinyl pyrrolidone as matrix materials. Controllable drug loading in needle tips was achieved by a two-step casting procedure. The needles were good in mechanical strength for penetrating the SC while presented excellent dissolving capability for releasing propranolol hydrochloride. In comparison with the solution counterpart, irrespective of being applied to intact skin or solid MNs-pretreated skin, dissolving MNs significantly increased the permeability and skin retention of propranolol. In conclusion, dissolving MNs could be a potential approach for enhancing dermal delivery of propranolol to treat IH.

Author(s):  
Prasetyanugraheni Kreshanti ◽  
Nandya Titania Putri ◽  
Valencia Jane Martin ◽  
Chaula Luthfia Sukasah

2017 ◽  
Vol 59 (8) ◽  
pp. 869-877 ◽  
Author(s):  
Tsuyoshi Kaneko ◽  
Satoru Sasaki ◽  
Naoko Baba ◽  
Katsuyoshi Koh ◽  
Kiyoshi Matsui ◽  
...  

2018 ◽  
Vol 2018 ◽  
pp. 1-6
Author(s):  
Chuan Wang ◽  
Qi Wang ◽  
Bo Xiang ◽  
Siyuan Chen ◽  
Fei Xiong ◽  
...  

Background. The aim of this study was to examine whether oral propranolol has any effect on neurodevelopment outcomes in young children with problematic infantile hemangiomas (IHs). Methods. Thirty-six children with a diagnosis of problematic IH who were treated with oral propranolol were compared with 34 healthy children with no history of propranolol therapy. Patients received propranolol therapy for at least 3 months. Gesell developmental schedules (GDS) were used to evaluate neurodevelopment outcomes in the two groups. The scores of each GDS domain were compared between the two groups. Results. There were no significant differences in developmental quotient (DQ) values for any of the five domains between the patients and healthy controls (P<0.05). Multiple stepwise regression analyses showed that none of the domains in the control group were influenced by the children’s gender or age (P<0.05). In addition, we found that gender, age at the initiation of therapy, age at the time of the neurodevelopment test, and treatment duration had no effect on any domain of the GDS in the patient group (P>0.05). Conclusion. Propranolol has no obvious effect on neurodevelopmental outcomes in children. Early treatment and treatment duration had no negative effect on central nervous system (CNS) development.


2019 ◽  
Vol 46 (5) ◽  
pp. 376-382
Author(s):  
Zhang Yu ◽  
Ren Cai ◽  
Lei Chang ◽  
Yajing Qiu ◽  
Xuanfeng Chen ◽  
...  

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2907
Author(s):  
Yanling Zhang ◽  
Majella E. Lane ◽  
David J. Moore

Polyethylene glycols (PEGs) and PEG derivatives are used in a range of cosmetic and pharmaceutical products. However, few studies have investigated the influence of PEGs and their related derivatives on skin permeation, especially when combined with other solvents. Previously, we reported niacinamide (NIA) skin permeation from a range of neat solvents including propylene glycol (PG), Transcutol® P (TC), dimethyl isosorbide (DMI), PEG 400 and PEG 600. In the present work, binary and ternary systems composed of PEGs or PEG derivatives combined with other solvents were investigated for skin delivery of NIA. In vitro finite dose studies were conducted (5 μL/cm2) in porcine skin over 24 h. Higher skin permeation of NIA was observed for all vehicles compared to PEG 400. However, overall permeation for the binary and ternary systems was comparatively low compared with results for PG, TC and DMI. Interestingly, values for percentage skin retention of NIA for PEG 400:DMI and PEG 400:TC were significantly higher than values for DMI, TC and PG (p < 0.05). The findings suggest that PEG 400 may be a useful component of formulations for the delivery of actives to the skin rather than through the skin. Future studies will expand the range of vehicles investigated and also look at skin absorption and residence time of PEG 400 compared to other solvents.


2020 ◽  
Vol 12 (1) ◽  
pp. 38-47 ◽  
Author(s):  
Lalit Kumar ◽  
Puneet Utreja

Objective: The objective of the present work was to develop transethosomes loaded with propranolol hydrochloride using Lipoid S100 as phospholipid, and oleic acid as permeation enhancer and evaluate them for prolonged release effect, in-vitro skin permeation, and in-vivo plasma concentration. Methods: Transethosomes loaded with propranolol hydrochloride were prepared by homogenization method. Furthermore, they were characterized by using Transmission Electron Microscopy (TEM), zeta sizer, Differential Scanning Calorimetry (DSC), and Confocal Laser Scanning Microscopy (CLSM) for in-vitro skin permeation. Plasma concentration profile of transethosomal gel was determined using Sprague Dawley rats and compared with a marketed oral tablet of propranolol hydrochloride. Results: Developed transethosomes loaded with propranolol hydrochloride showed acceptable size (182.7 ± 5.4 nm), high drug entrapment (81.98 ± 2.9%) and good colloidal characteristics [polydispersity index (PDI) = 0.234 ± 0.039, zeta potential = -21.91 ± 0.65 mV]. Transethosomes showed prolonged in-vitro release of propranolol hydrochloride for 24 h. Results of in-vitro skin permeation studies of transethosomal gel showed 74.34 ± 2.33% permeation of propranolol hydrochloride after 24 h and confocal microscopy revealed accumulation of transethosomes in the stratum basale layer of the skin. Transethosomal gel was capable to prolong the in-vivo release of propranolol hydrochloride upto 24 h. The value of peak plasma concentration (Cmax) of propranolol hydrochloride was found to be 93.8 ± 3.6 ng/mL which was very high compared to the marketed oral tablet of propranolol hydrochloride (45.6 ± 3.1 ng/mL). Conclusion: The results suggested that transethosomal gel of propranolol hydrochloride could be a better alternative to oral propranolol hydrochloride as it can avoid various disadvantages of oral propranolol hydrochloride like high dosing frequency, first pass effect, and organ toxicity.


2015 ◽  
Vol 62 (2) ◽  
pp. 518-519 ◽  
Author(s):  
C. Léauté-Labréze ◽  
P. Hoeger ◽  
J. Mazereeuw-Hautier

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