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Insoluble drug delivery strategies: review of recent advances and business prospects
Open accessAbstract
The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.
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“About 90% of preclinical small molecule candidate drugs have poor solubility, so the realization of this process is very challenging.282”
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Metadata
- Authors
- Kalepu, S., & Nekkanti, V.
- Affiliations
- Western University of Health Sciences (US)
- Corresponding author
- Kalepu, Sandeep
- Venue
- Acta Pharmaceutica Sinica B
- Publisher
- Elsevier BV
- Published
- 2015-09
- Volume
- 5
- Issue
- 5
- Pages
- 442-453
- ISSN
- 2211-3835 (ISSN-L)
- PMC
- PMC4629443
- OpenAlex
- W1195955210
- Cited by
- 1,410
- References
- 86
- Citations by year
- 2026: 111 · 2025: 140 · 2024: 148 · 2023: 166 · 2022: 155 · 2021: 179 · 2020: 191 · 2019: 139 · 2018: 95 · 2017: 62 · 2016: 20 · 2015: 2
- FWCI
- 6.68
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Acta Pharmaceutica Sinica B (publishedVersion, cc-by-nc-nd)
- Europe PMC (PubMed Central) (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- poorly water-soluble drugs, drug solubility, bioavailability, drug formulation, drug reformulation, pharmaceutical patents, marketing exclusivity, lipophilic drugs, high molecular weight drugs
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