Indian Contribution to Design and Development of SMEDDS

 

Dr. Shoaib Ahmad

University School of Pharmaceutical Sciences, Rayat-Bahra University, Mohali 140104 India

 

 

ABSTRACT:

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.

 

 

 

 

INTRODUCTION:

The self-microemulsifying drug delivery system (SMEDDS) represents one of the novel drug delivery systems. These systems help in overcoming a number of issues related to solubility, absorption, drug targeting etc. The present article attempts to present the contribution of Indian scientists and academicians in this promising field.  SMEDDS of lipophilic drugs have been reviewed¹. A detailed strategy for enhanced therapeutic profile of SMEDDS has been presented². Approaches of lipid-based delivery system such as SMEDDS for lymphatic targeting have been reviewed³.

 

SMEDDS for polyphenols were discussed⁴. Pharmacokinetics and IVIVC potential of lipid-based formulations including SMEDDS have been reviewed⁵. The challenges in SMEDDS formulation and development have been reviewed⁶. The importance of component selection in the SMEDDS formation has been highlighted⁷. The design and development of SMEDDS for colonic drug delivery has been reported⁸. Midha et al. (2016) recently reviewed the prospective of SMEDDS⁹.

 

Indian Contribution in Designing and Developing SMEDDSL:

Design of celecoxib SMEDDS has been tried in order to improve oral bioavailability of the drug. Using PEG-8 caprylic/capric glycerides, Tween 20 and Propylene glycol monocaprylic ester, the team was able to enhance relative bioavailability to an extent of 132% as compared to the drug bioavailability from conventional capsule¹⁰. SMEDDS of fenofibrate has been reported. Using Labrafac CM10, Tween 80 and polyethylene glycol 400, they were able to achieve complete release of drug in just 15 minutes¹¹. SMEDDS of acyclovir has been prepared using Tween 60, glycerol and sunflower oil. The absorption of drug from SMEDDS form was 350 % higher than the same of the pure acyclovir solution¹². SMEDDS of ritonavir has also been reported. These SMEDDS utilised Imwitor 988, Cremophor EL / RH 40 and Capmul GMS K-50¹³. SMEDDS of tacrolimus has been designed and later, demonstrated better immunosuppressant action in mice than Pangraf capsules used as reference¹⁴. SMEDDS of tacrolimus has been prepared using ethyl oleate, Solutol HS 15 and glycofurol; for intravenous administration¹⁵. SMEDDS formulation strategies for tacrolimus has been discussed¹⁶. Rice germ oil has been used in SMEDDS of tacrolimus.  It had better dissolution and hence, better pharmacokinetic profile¹⁷.

 

SMEDDS of beta-Artemether using natural lipophile  and Capryol 90 has been developed. This SMEDDS had better anti-malarial activity as compared to the marketed formulation (Larither)¹⁸. SMEDDS of exemestane has been developed¹⁹. Oral bioavailability of exemestane has been enhanced through SMEDDS²⁰. SMEDDS of glyburide has been designed using cosurfactant (Transcutol P)²¹. Bicalutamide SMEDDS has been developed and found almost 200 % increase in the relative bioavailability of bicalutamide SMEDDS when compared with suspension of the same drug²². Valsartan SMEDDS has been prepared using Capmul MCM, Tween 80 and PEG 400.  The SMEDDS had better oral bioavailability²³. The therapeutic potential of SMEDDS of curcumin in inflammation, cancer, AIDS, and cardiovascular / neurological disorders has been pointed out²⁴. SMEDDS of candesartan cilexetil has been prepared. Better drug dissolution was observed in comparison to commercial tablet²⁵.

 

SMEDDS of lovastatin has been reported²⁶. The therapeutic potential of lovastatin SMEDDS for oral administration has been highlighted²⁷. SMEDDS of Atorvastatin calcium using Capmul MCM has been developed²⁸. SMEDDS of atorvastatin using hydrophilic carriers has been developed²⁹. Therapeutic potential of silymarin SMEDDS has been discussed³⁰. Thakkar et al. (2011) formulated and characterized SMEDDS of raloxifene with better oral bioavailability³¹. Chaurasiya et al. (2012) reported SMEDDS of paclitaxel and docetaxel which used elacridar for effective transport of drugs across intestinal epithelium model³². Shete et al. (2015) reported SMEDDS for cytosolic delivery of antineoplastics such as etoposide³³. Oleic acid has been used in SMEDDS of furosemide which had negligible hemolytic potential³⁴.SMEDDS of domperidone has been developed using Labrafac CC, Tween 80 and Transcutol. Improvement in oral bioavailability of the drug from SMEDDS was observed³⁵. SMEDDS for terbinafine has been developed which exhibited a potential for better lymphatic uptake³⁶. SMEDDS of noscapine has been prepared with enhanced oral bioavailability³⁷.

 

CONCLUSIONS:

SMEDDS are a popoular novel drug delivery systems and they can help in overcoming a number of problems related to solubility, pharmcokinetics, drug targeting etc. They assume significance in case of lipophilic drugs. A strategy for enhanced therapeutic profile of SMEDDS has been suggested. SMEDDS has been successful for lymphatic targeting. There are still more  challenges in SMEDDS formulation and development.

 

ACKNOWLEDGEMENTS:

Author acknowledges the support from Dr. Shibli J. Ahmad, Jamia Hamdard, New Delhi; author's  family and Rayat-Bahra University, Mohali.

 

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Received on 07.03.2017        Modified on 20.04.2017

Accepted on 10.05.2017     ©A&V Publications All right reserved