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Related Concept Videos

Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

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Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
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Glucagon-like Receptor Agonists01:24

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
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Drug Delivery: Miscellaneous Routes01:22

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Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
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Local Anesthetics: Chemistry and Structure-Activity Relationship01:27

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Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
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Insulin-replacement therapy usually includes both long-acting insulin (basal) and short-acting insulin (to cater to postprandial needs). In a diverse group of type 1 diabetes patients, the average daily insulin dose is typically 0.5-0.7 units/kg body weight. However, obese patients and pubertal adolescents may need more due to insulin resistance.
The basal dose constitutes about 40%-50% of the total daily dose, with the rest as premeal insulin. The mealtime insulin dose should mirror...
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Insulin: Biosynthesis, Chemistry, and Preparation01:25

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The endoplasmic reticulum (ER) of pancreatic β-cells synthesizes preproinsulin, which consists of a signal peptide, A and B chains, and a C-peptide. Preproinsulin is then cleaved and folded into proinsulin, which translocates to the Golgi apparatus for sorting and packaging into secretory granules. In these granules, enzymatic clipping generates insulin and C-peptide.
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PLGA-based long-acting injectable (LAI) formulations.

Kinam Park1

  • 1Purdue University, Weldon School of Biomedical Engineering and Department of Industrial and Molecular Pharmaceutics, West Lafayette, IN 47907, USA; Akina, Inc., 3495 Kent Avenue, West Lafayette, IN 47906, USA.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|April 23, 2025
PubMed
Summary

Advancements in characterizing poly(lactide-co-glycolide) (PLGA) polymers and understanding drug release mechanisms are improving long-acting injectable (LAI) formulations. This shift enables a move from trial-and-error to a Quality by Design approach, with AI offering future potential.

Keywords:
Artificial intelligenceCharacterization of PLGA polymersDrug release mechanismsFDA approvalLong-acting injectable (LAI) formulationsQuality by design (QbD)

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Long-acting injectable (LAI) formulations have been utilized for over 30 years, with poly(lactide-co-glycolide) (PLGA) polymers being the predominant excipient in approved products.
  • Traditional development of PLGA-based LAI formulations has been hindered by a lack of comprehensive understanding of formulation complexities and inadequate analytical methods for polymer characterization.

Purpose of the Study:

  • To provide a perspective on recent advancements in characterizing PLGA polymers within final LAI products.
  • To enhance understanding of drug release mechanisms in LAI products.
  • To explore the potential of artificial intelligence (AI) in advancing LAI formulation development.

Main Methods:

  • Review of recent analytical advancements for characterizing PLGA polymers in finished LAI formulations.
  • Analysis of drug release mechanisms associated with LAI products.
  • Discussion on the integration of Quality by Design (QbD) principles.
  • Exploration of AI applications in formulation science.

Main Results:

  • Improved characterization techniques offer deeper insights into PLGA polymer properties within LAI products.
  • Enhanced understanding of drug release kinetics and influencing factors.
  • The transition from empirical trial-and-error to a systematic QbD approach is facilitated by these advancements.
  • AI presents emerging opportunities to refine and accelerate LAI formulation development.

Conclusions:

  • Advanced characterization and mechanistic understanding are crucial for optimizing PLGA-based LAI formulations.
  • A shift towards QbD, supported by AI, promises more efficient and predictable LAI product development.
  • Future research should focus on leveraging these advancements for innovative LAI therapies.