Poly(lactic acid)/poly(lactic-co-glycolic acid)-based microparticles: an overview
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Poly(glycolic acid), poly(lactic acid) and poly(lactic-co-glycolic acid) were approved by the United States Food and Drug Administration (FDA) in the 1970s as materials for the manufacturing of bioresorbable surgical sutures, but soon became the reference materials for the preparation of sustained release formulations, especially injectable microparticles. Since the 1986 approval of Decapeptyl® SR, the first product based on PLGA microspheres, more than 15 such products have been approved for clinical use.
This article highlights the key steps that brought to the development of injectable poly(lactic acid)/poly(lactic-co-glycolic acid) microparticles for the sustained release of active pharmaceutical ingredients. After a brief history of some pioneering works that opened the field of controlled drug delivery, the key steps that led to the development of these polymers and the approval of the first microparticle-based medicinal products are reviewed. Finally, the general characteristics of these polymers are described and the classical preparation method is explained.
Poly(lactic acid)/poly(lactic-co-glycolic acid) microparticles are among the most successful drug delivery systems. The recent approval of new medicinal products based on PLGA microspheres is the proof that pharmaceutical companies have continued to exploit this drug delivery technology. The possible development of generics and the continuous discovery of therapeutic peptides will hopefully further the success of microsphere technology.
KeywordsMicrospheres Drug delivery systems Long-acting injections PGA PLA PLGA
The author would like to thank Sheila Beatty for editing the English usage in the manuscript.
Compliance with ethical standards
Conflict of interest
The author declares no conflicts of interest.
Statement of human and animal rights
This article does not contain any studies with human and animal subjects performed by the author.
- American Pharmaceutical Review (2018) Perseris now available in the U.S. for the treatment of schizophrenia in adults. https://www.americanpharmaceuticalreview.com/1315-News/355892-Perseris-Now-Available-in-the-U-S-for-the-Treatment-of-Schizophrenia-in-Adults/. Accessed 21 Nov 2018
- Benita S (1996) Microencapsulation—methods and industrial application. Marcel Dekker, New YorkGoogle Scholar
- Boswell GA, Scribner RN (1973) Polylactide-drug mixtures. US3773919AGoogle Scholar
- Burgess DJ, Wright JC (2012) An introduction to long acting injections and implants. In: Wright JC, Burgess DJ (eds) long acting injections and implants. Springer, Berlin, pp 1–9Google Scholar
- Helfand WH, Cowen DL (1983) Evolution of pharmaceutical oral dosage forms. Pharm Hist 25:3–18Google Scholar
- Indivior (2019) Indivior announces launch of PERSERISTM (risperidone) for the treatment of schizophrenia in adults. http://www.indivior.com/wp-content/uploads/2019/02/PERSERIS-Launch-Press-Release_FINAL_2.26.19.pdf. Accessed 15 Mar 2019
- Janssen Pharmaceuticals (2019) RISPERDAL CONSTA® Highlights of prescribing information. http://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/RISPERDAL+CONSTA-pi.pdf. Accessed 15 Mar 2019
- Karlsson I (2017) Injectable drug delivery: devices meet next-generation formulations. ONdrugDelivery Magazine 75:22–25Google Scholar
- Kissel T, Rummelt A (1990) Microspheres for depot-injection: parlodel LAR®a once-a-month delivery system for bromocriptine. Bull Tech Gattefosse Rep 83:71–82Google Scholar
- Lu Y, Park K (2012) Microencapsulation: Methods and Pharmaceutical Applications. In: Encyclopedia of Pharmaceutical Science and Technology, 4th edn. Informa Healthcare, USAGoogle Scholar
- Ranger GO (1974) Microencapsulation—a brief history and introduction. In: Vandegaer JE (ed) Microencapsulation—processes and applications. Plenum Press, New York, pp 1–20Google Scholar
- Ratner BD, Hoffman AS, Schoen FJ, Lemons JE (2013) Biomaterials science—an introduction to materials in medicine, 3rd edn. Academic Press, CambridgeGoogle Scholar
- Reich G (1997) Use of DSC to study the degradation behavior of PLA and PLGA microparticles. Drug Dev Ind Pharm 23(1177):1189Google Scholar
- Scheindlin S (2001) A brief history of pharmacology. Mod Drug Discov 4(87–88):91Google Scholar
- Schmitt EE, Polistina RA (1967) Surgical sutures. US3297033AGoogle Scholar
- Schneider AK (1955) Polymers of high melting lactide. US2703316AGoogle Scholar
- Tice TR (2017) A 30-year history of PLG applications in parenteral controlled drug release. Pharm Technol 41:26–32Google Scholar
- Wang Y, Qu W, Choi SH (2017) FDA’s regulatory science program for generic PLA/PLGA-based drug products. Am Pharm Rev 19(4):5–9Google Scholar
- Wu XS (1995) Synthesis and properties of biodegradable lactic/glycolic acid polymers. In: Wise DL, Trantolo DJ, Altobelli DE, Yaszernski MJ, Gresser JD et al (eds) Encyclopedic handbook of biomaterials and bioengineering. Marcel Dekker, New York, pp 1015–1054Google Scholar