A SYSTEMATIC REVIEW ON SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEMS: A POTENTIAL STRATEGY FOR DRUGS WITH POOR ORAL BIOAVAILABILITY

G V Radha,Sadhana Burada,K Trideva Sastri,Jampala Rajkumar

doi:10.22159/ijap.2019v11i1.29978

G V Radha, Sadhana Burada + Show 2 more

Open Access

https://doi.org/10.22159/ijap.2019v11i1.29978

Copy DOI

Abstract

Currently a marked interest in developing lipid-based formulations to deliver lipophilic compounds. Self-emulsifying system has emerged as a dynamic strategy for delivering poorly water-soluble compounds. These systems can embrace a wide variety of oils, surfactants, and co-solvents. An immediate fine emulsion is obtained on exposure to water/gastro-intestinal fluids. The principal interest is to develop a robust formula for biopharmaceutical challenging drug molecules. Starting with a brief classification system, this review signifies diverse mechanisms concerning lipid-based excipients besides their role in influencing bioavailability, furthermore pertaining to their structured formulation aspects. Consecutive steps are vital in developing lipid-based systems for biopharmaceutical challenging actives. Such a crucial structured development is critical for achieving an optimum formula. Hence lipid excipients are initially scrutinized for their solubility and phase behavior, along with biological effects. Blends are screened by means of simple dilution test and are consequently studied with more advanced biopharmaceutical tests. After discerning of the principle formula, diverse technologies are offered to incorporate the fill-mass either in soft/hard gelatin capsules. There is also feasibility to formulated lipid-system as a solid dosage form. Although such solid technologies are desirable but such should not undermine the biopharmaceutical potential of lipid-formulations.

Highlights

With today’s contemporary drug discovery techniques, innovating drug candidates without compromising on safety and efficacy is a challenge
The results revealed that the principal reason for improved bioavailability was due to enhanced solubilization and permeability of the drug in the lipid-rich pre-absorptive intestinal environment [93]
A significant opportunity along with a potential challenge is anticipated from most insoluble drug molecules approved by Food and Drug Administration (FDA), besides those in the development stage

Summary

INTRODUCTION

With today’s contemporary drug discovery techniques, innovating drug candidates without compromising on safety and efficacy is a challenge. Type I lipid-based drug delivery system (LBDDS) include only triglyceride oil or with certain mixtures with its glycerides Formulations belonging to this category potentially do not self-disperse, it requires bile salts, lipolysis products and phospholipids to lower interfacial tension post administration [14]. Since medium chain triglycerides prominently have high solvent capacity not susceptible to oxidation, they are potentially employed in lipid-based formulation systems [42, 43]. Few drugs are poorly water solubility as a result of their lipophilicity Such molecules possess higher value about 2-4 of the partition coefficient (logP), are usually suitable candidates for lipid-based systems. Dissolution, intestinal membrane methods (cell culture and isolated animal tissue models) along with lipolysis of the lipid excipient are several in vitro techniques and are prominently employed to evaluate lipid-based formulations [98]. Topotecan HCl (Hycamtin®) Loratadine (Claritin®) Isotretinoin (Absorica®) Enzalutamide (Xtandi®) Nintedanib (Ofev®) Calcifediol (RayaldeeTM)

IIIA IV I I III

Findings

CONCLUSION