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Preclinical Formulations: Insight, Strategies, and Practical Considerations

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Abstract

A lot of resources and efforts have been directed to synthesizing potentially useful new chemical entities (NCEs) by pharmaceutical scientists globally. Detailed physicochemical characterization of NCEs in an industrial setup begins almost simultaneously with preclinical testing. Most NCEs possess poor water solubility posing bioavailability issues during initial preclinical screening, sometimes resulting in dropping out of an NCE with promising therapeutic activity. Selection of right formulation approach for an NCE, based on its physicochemical properties, can aid in improving its solubility-related absorption and bioavailability issues. The review focuses on preclinical formulations stressing upon different preclinical formulation strategies and deciphers the understanding of formulation approaches that could be employed. It also provides detailed information related to a vast pool of excipients available today, which is of immense help in designing preclinical formulations. Few examples mentioned, throw light on key aspects of preclinical formulation development. The review will serve as an important guide for selecting the right strategy to improve bioavailability of NCEs for academic as well as industrial formulation scientists.

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Abbreviations

NCE:

New chemical entity

FIH:

first in human

API:

active pharmaceutical ingredient

GLPs:

good laboratory practices

GIT:

gastrointestinal tract

SNEDDs:

self nano-emulsifying drug delivery systems

CTAB:

cetyl trimethyl ammonium bromide

CPC:

cetyl pyridinium chloride

LCTs:

long-chain triglycerides

MCTs:

medium-chain triglycerides

SCTs:

short-chain triglycerides

DMPK:

drug metabolism and pharmacokinetics

SOP:

standard operating procedure

DSC:

differential scanning calorimetry

TGA:

thermogravimetric analysis

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Acknowledgments

Sanket M. Shah and Ankitkumar S. Jain are thankful to Piramal Enterprise Limited, Mumbai, India for providing financial assistance.

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Authors declare no conflict of interest.

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Authors and Affiliations

  1. Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, 400098, India

    Sanket M. Shah, Ankitkumar S. Jain & Mangal S. Nagarsenker

  2. Preformulation and Formulation Development, Piramal Enterprise Limited, Goregaon, Mumbai, 400063, India

    Ritu Kaushik & Maneesh J. Nerurkar

Authors
  1. Sanket M. Shah
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  2. Ankitkumar S. Jain
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  3. Ritu Kaushik
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  4. Mangal S. Nagarsenker
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  5. Maneesh J. Nerurkar
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Corresponding author

Correspondence to Mangal S. Nagarsenker.

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Sanket M. Shah and Ankitkumar S. Jain have contributed equally to the article.

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Shah, S.M., Jain, A.S., Kaushik, R. et al. Preclinical Formulations: Insight, Strategies, and Practical Considerations. AAPS PharmSciTech 15, 1307–1323 (2014). https://doi.org/10.1208/s12249-014-0156-1

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  • DOI: https://doi.org/10.1208/s12249-014-0156-1

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