Alginate-based drug oral targeting using bio-micro/nano encapsulation technologies

ABSTRACT

Introduction

Oral delivery is the most common administrated drug delivery path. However, oral administration of lipophilic drugs has some limitations: they have poor dose-response due to low and varied dissolution kinetics and oral bioavailability with sub-optimal dissolution within the aqueous gastrointestinal microenvironment. Therefore, there is a need for robust formulating methods that protect the drug until it reaches to its optimum absorption site, allowing its optimum pharmacological effects via increasing its intestinal permeation and bioavailability.

Area covered

Herein, we provide insights on orally administered lipophilic drug delivery systems. The detailed description of the obstacles associated with the oral bioavailability of lipophilic drugs are also discussed. Following this, techniques to overcome these obstacles with much emphasis on optimal safety and efficacy are addressed. Newly designed ionic vibrational jet flow encapsulation technology has enormous growth in lipophilic drug delivery systems, which is discussed thereafter.

Expert opinion

Researchers have shown interest in drug’s encapsulation. A combination of drug-bile acid and microencapsulation methods can be one promising strategy to improve the oral delivery of lipophilic drugs. However, the most critical aspect of this approach is the selection of bile acids, polymer, and encapsulation technology.

KEYWORDS:

• Bioavailability
• encapsulation
• gastrointestinal tract
• ionic jet flow technology
• lipophilic drugs
• microcapsules
• oral administration

Article highlights

• Lipophilic drugs are poorly water-soluble but dissolve readily in lipids and rapidly growing in the drug market despite its low bioavailability and poor water-solubility.

• Oral delivery is the most common method of drug delivery, mainly due to comfort and patient compliance. However, orally administered drugs have to pass via many biochemical and physiological obstructions and eventually decrease the bioavailability of drugs.

• The human intestine expresses an abundant amount of cytochrome P450 iso-enzymes like cytochrome P-450 3A (CYP 3A4) act as a primary barrier for the absorption of lipophilic drugs. Also, efflux proteins are mainly present in the intestinal membrane, where they can expel a range of structurally different drugs, drug conjugates, and metabolites.

• There are numerous techniques and strategies to improve oral bioavailability, and one of them is the drug’s encapsulation technique.

• Ionic Gelation Vibrational Jet Flow technology (IGVJF) in drug delivery is one of the newly pioneered physio-chemical microencapsulation methods for medical and biotechnological applications.

• Recent roles of bile acids are expanded towards the importance of microcapsules- stabilization and as permeation-enhancing agent for the optimal bioavailability of lipophilic drugs.

This box summarizes key points contained in the article.

Declaration of interest

H Al-Salami’s work is partially supported by the European Union’s Horizon 2020 SALSETH research and innovation programme under the Marie Sklodowska-Curie Grant agreement No. 872,370. H Al-Salami has been and is currently receiving funding from the Beijing Nat-Med Biotechnology Co. Ltd. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the paper apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose

Additional information

Funding

H Al-Salami has been and is currently receiving funding from Beijing Nat-Med Biotechnology Co. Ltd.