Development Of Self-microemulsifying Drug Delivery System Research Articles

Indian contribution to design and development of SMEDDS

The self-microemulsifying drug delivery system (SMEDDS) are one of the novel drug delivery systems. SMEDDS help in overcoming a number of formulation-related issues such as solubility, absorption, drug targeting etc. Indian scientists and acdemicians have made significant and substantial contribution to design and developments of SMEEDS. Lipophilic, anti-cancer, anti-hyperlipidemic, anti-viral drugs have been quite popular for development of SMEDDS. Approaches have been suggested and experimentally proven that SMEDDS in many cases have enhanced therapeutic profiles. SMEDDS for polyphenols have been developed. Pharmacokinetics and IVIVC potential of SMEDDS has also been discussed. The Indians community has worked on design and development of SMEDDS of synthetic drugs such as celecoxib, acyclovir, ritonavir, tacrolimus, exemestane, bicalutamide, valsartan, candesartan cilexetil, etc. have been developed. Similarly SMEDDS of natural origin drugs such as beta-Artemether, curcumin, lovastatin, atorvastatin, silymarin, paclitaxel, docetaxel, etoposide etc. have also been prepared. SMEDDS has been successfully tried for lymphatic targeting of drugs. Still, here are still more challenges ahead in SMEDDS formulation and development. The present article attempts to outline the contribution of Indians in this promising field.

Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems (SMEDDSs) for oral delivery of aciclovir

The study investigated the influence of formulation parameters for design of self-microemulsifying drug delivery systems (SMEDDSs) comprising oil (medium chain triglycerides) (10%), surfactant (Labrasol®, polysorbate 20, or Kolliphor® RH40), cosurfactant (Plurol® Oleique CC 497) (q.s. ad 100%), and cosolvent (glycerol or macrogol 400) (20% or 30%), and evaluate their potential as carriers for oral delivery of a poorly permeable antivirotic aciclovir (acyclovir). The drug loading capacity of the prepared formulations ranged from 0.18–31.66mg/ml. Among a total of 60 formulations, three formulations meet the limits for average droplet size (Z-ave) and polydispersity index (PdI) that have been set for SMEDDSs (Z-ave≤100nm, PdI<0.250) upon spontaneous dispersion in 0.1M HCl and phosphate buffer pH 7.2. SMEDDSs with the highest aciclovir loading capacity (24.06mg/ml and 21.12mg/ml) provided the in vitro drug release rates of 0.325mgcm−2min−1 and 0.323mgcm−2min−1, respectively, and significantly enhanced drug permeability in the parallel artificial membrane permeability assay (PAMPA), in comparison with the pure drug substance. The results revealed that development of SMEDDSs with enhanced drug loading capacity and oral delivery potential, required optimization of hydrophilic ingredients, in terms of size of hydrophilic moiety of the surfactant, surfactant-to-cosurfactant mass ratio (Km), and log P of the cosolvent.

Development of SMEDDS using natural lipophile: Application to β-Artemether delivery

The objective of the present investigation was to formulate self-microemulsifying drug delivery systems (SMEDDS) using a novel, indigenous natural lipophile (N-LCT) as an oily phase. SMEDDS based on N-LCT and commercially available modified oil (Capryol 90) were formulated and their application in improving the delivery of a lipophilic anti-malarial drug, β-Artemether (BAM) was also evaluated. BAM-loaded SMEDDS were characterized with respect to mean globule size and in vitro drug release profile in comparison to the marketed formulation (Larither ®). Comparative in vivo anti-malarial performance of the developed SMEDDS was evaluated against the (Larither ®) in Swiss male mice infected with lethal ANKA strain of Plasmodium berghei. The parameters studied were percent parasitemia, activity against time and animal survival period. Both the BAM–SMEDDS showed excellent self-microemulsification efficiency and released >98% of the drug in just 15 min whereas (Larither ®) showed only 46% drug release at the end of 1 h. The mean globule size for optimized BAM–SMEDDS was <100 nm. The anti-malarial studies revealed that BAM–SMEDDS resulted in significant improvement in the anti-malarial activity ( P < 0.05) as compared to that of (Larither ®) and BAM solubilized in the oily phases and surfactant. The developed SMEDDS highlight safety for use and potential applications of indigenous natural lipophile in the development of novel colloidal drug carriers.