Preparation and Evaluation of Cubic Nanoparticles for Improved Transdermal Delivery of Propranolol Hydrochloride
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Research Article Preparation and Evaluation of Cubic Nanoparticles for Improved Transdermal Delivery of Propranolol Hydrochloride Lingjun Zeng,1 Chun Tao,1 Zhihong Liu,1 Jing Zhang,1 Minxin Zhang,1 Jialiang Zhang,1 Shengnan Fang,1 Xiaoyu Ma,2 Hongtao Song,1,3 and Xin Zhou1
Received 21 March 2020; accepted 2 September 2020 Abstract. Transdermal drug delivery of propranolol hydrochloride (PRH) is promising for the treatment of infantile hemangioma (IH). Clinically used PRH hydrogel fails to reach the deep IH for complete recovery. In this study, the PRH-loaded cubic nanoparticles (CNPs) were prepared to promote the transdermal effect of PRH. A remote drug loading method was developed to prepare the PRH-CNPs. For the traditional passive drug loading method, the largest encapsulation efficiency (EE%) was around 50%. The remote drug loading was performed by increasing the pH of the mixture of blank CNPs and PRH solution. The optimal PRH-CNPs showed an EE% of 90.15 ± 2.44% at pH 8.5. The permeation of the PRH solution was poor while the PRH-CNPs showed greatly enhanced skin permeation. It was found that smaller-sized PRH-CNPs contributed to increased skin permeation and retention. In addition, the PRH-CNPs had higher cytotoxicity towards the EOMA cells when compared with the PRH solution. During storage for 1 month, the PRH-CNPs kept stable size distribution, pH, and EE%. In conclusion, results of this study suggested that the PRHCNPs could be a potential candidate for the treatment of the IH by transdermal delivery. KEY WORDS: cubic nanoparticles; propranolol hydrochloride; remote drug loading; transdermal.
INTRODUCTION Infantile hemangioma (IH) is one of the most common benign vascular tumors seen during infancy [1]. About 4% of infants may suffer from IH. It is usually not fatal and can be self-healed. However, the healing process may last for several years [2]. Moreover, the IH that distributes on conspicuous parts of the body like the face may result in heavy psychological pressure. Thus, it is vital to develop a safe and effective treatment for IH. Propranolol hydrochloride (PRH) is a nonselective β-adrenergic blocker which is clinically approved for antihypertensive and antiarrhythmic, was found to be dramatically effective for IH in 2008 [3]. Oral administration of PRH is now the first-line treatment for IH [4]. However, it may cause various adverse effects including
Lingjun Zeng and Chun Tao contributed equally to this work. Electronic supplementary material The online version of this article (https://doi.org/10.1208/s12249-020-01809-7) contains supplementary material, which is available to authorized users. 1
Department of Pharmacy, Fuzong Clinical Medical College of Fujian Medical University (900 Hospital of the Joint Logistics Team), Fuzhou, 350025, People’s Republic of China. 2 College of Pharmacy, Fujian Medical University, Fuzhou, 350108, People’s Republic of China. 3 To whom correspondence should be addressed. (e–mail: [email protected])
diarrhea, bradycardia, sleep disturbance, bronchospasm, and hypoten
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