Research Article: Development and Characterization of Nanostructured Pharmacosomal Mesophases: An Innovative Delivery System for Bioactive Peptides

Date Published: November 29, 2018

Publisher: Tabriz University of Medical Sciences

Author(s): Maryam Rezvani, Javad Hesari, Seyed Hadi Peighambardoust, Maria Manconi, Hamed Hamishehkar.


Purpose: To potentially enhance the bioavailability and extend the bioactivity effectiveness of Isoleucine-Proline-Proline (IPP, an antihypertensive bioactive peptide of dairy origin), a novel Lyotropic Liquid Crystalline Pharmacosomal Nanoparticle (LLCPNP) was synthesized, and its physicochemical and technological characteristics were studied.

Partial Text

In recent decades, application of the Lyotropic Liquid Crystals (LLCs) in the field of drug delivery has gained considerable attraction from many scientists and research communities.1-6 The unique and peculiar physicochemical and structural characteristics of LLCs, similarity to the bio-systems and providing superior advantages than traditional delivery systems are the causes of this scientific interest. These structures are considered as an intermediate state of matter between a crystalline solid (consisting the long-range positional and orientational order in three dimensions) and an isotropic liquid (with no long-range order), which need a solvent to be formed. This state may simultaneously represent the crystal mechanical stability and liquid fluidity.7-9 These mesophases have been utilized to protect and deliver some molecules with different biological activities such as immunosuppressive and anticancer agents, antibiotics and vitamins.10-12 Regarding the importance of bioactive peptides in biopharmaceutical applications, the employment of LLCs should be considered as a noteworthy method for delivery of these valuable compounds. Isoleucine-Proline-Proline (IPP) is an antihypertensive bioactive peptide with dairy origin. Hypertension is the most effective risk factor causing cardiovascular disease (CVD), which has become an important global public health concern and will change to the leading cause of death in subsequent years. In addition, high blood pressure is the cause of many other Illnesses, including kidney failure, stroke and premature death.13 Angiotensin I-converting enzyme (ACE) plays a key role in this regard. This enzyme can raise blood pressure through catalyzing the conversion of angiotensin I to angiotensin II and vasoconstriction.14 Many of the antihypertensive drugs inhibit this process, but these synthetic ACE inhibitors have numerous side effects. In recent years, some peptides with food origin have shown ACE inhibitory properties. The utilization of these bioactive peptides reduces the cost of hypertension treatment and adverse side effects.15-18 In this regard, the function of IPP has been prominent, but its undesirable pharmacokinetics, including low bioavailability, short half-life, rapid clearance from the body and probable interaction with the other components in oral delivery formulations necessitate the need for nanoencapsulation of this bioactive peptide.19 On the other hand, the chemical structure of this molecule makes it appropriate to produce specific LLCs, Lyotropic Liquid Crystalline Pharmacosomal Nanoparticles (LLCPNPs), via complex formation (Figure 1).

The successful preparation technique and appropriate physicochemical characteristics of LLCPNPs containing IPP acquired in this work can be applicable for the similar compounds. According to the results of the SAXS and PLM, these nanoparticles can be classified as lamellar LLC phases. As illustrated in this research, the utilization of this nanocarrier type in peptide delivery can increase the patient tolerance and decrease the dosage and administration frequency of the peptide via the steady plasma concentration maintenance at the desired therapeutic level for a longer period. The peptide release from these novel LLCs is independent of the carrier membrane fluidity, leading to sustained release of IPP. This feature along with the bioavailability promotion can result in the promising potential for manufacturing the biopharmaceutical and nutraceutical products aiming at preventing and controlling the diseases originated from hypertension and can improve the health.

The present paper does not contain any studies involving animals or human participants.

There are no conflicts to declare.




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