Standard Operating Procedure for Development of Nanoparticle Formulations for Oral Delivery
1) Purpose
The purpose of this SOP is to outline the procedure for developing nanoparticle-based formulations for oral drug delivery. Nanoparticles offer improved bioavailability, protection of the active pharmaceutical ingredient (API) from the harsh gastrointestinal (GI) environment, and targeted drug release.
2) Scope
This SOP applies to personnel involved in the development, formulation, and characterization of nanoparticles intended for oral drug delivery, particularly in pharmaceutical research and formulation development settings.
3) Responsibilities
- Operators: Responsible for preparing and optimizing nanoparticle formulations for oral delivery.
- QA: Ensures that the nanoparticles meet the required specifications for particle size, stability, drug release, and GI compatibility.
4) Procedure
4.1 Selection of Materials
4.1.1 Polymer and Lipid Selection
- 4.1.1.1 Use biodegradable polymers (e.g., PLGA, chitosan) or lipids (e.g., solid lipid nanoparticles) that are compatible with oral administration and provide protection against the GI environment.
4.1.2 Drug Selection
- 4.1.2.1 Choose the API based on its stability in the GI tract, solubility, and suitability for nanoparticle encapsulation. Consider using prodrugs or enzyme inhibitors to improve bioavailability if necessary.
4.2 Nanoparticle Preparation
4.2.1 Emulsification or Nanoprecipitation Method
- 4.2.1.1 Prepare nanoparticles using emulsification, nanoprecipitation, or other suitable methods. Aim for a particle size of 100–300 nm to
optimize absorption in the GI tract.
4.2.2 Encapsulation of Drug
- 4.2.2.1 Encapsulate the drug within the nanoparticle core during synthesis to protect it from degradation in the acidic environment of the stomach.
4.3 Characterization and Testing
4.3.1 Particle Size and Surface Charge
- 4.3.1.1 Measure the particle size using dynamic light scattering (DLS) and determine the zeta potential to ensure stability in gastrointestinal fluids.
4.3.2 Drug Loading and Encapsulation Efficiency
- 4.3.2.1 Quantify the amount of drug encapsulated in the nanoparticles using UV-Vis spectrophotometry or high-performance liquid chromatography (HPLC). Calculate encapsulation efficiency to ensure that the drug loading meets the desired specifications.
4.3.3 In Vitro Release Studies
- 4.3.3.1 Perform in vitro drug release studies using simulated gastrointestinal fluids to assess how the drug is released from the nanoparticles in different sections of the GI tract (e.g., stomach, intestine).
4.3.4 Stability Testing
- 4.3.4.1 Conduct stability studies under different environmental conditions (e.g., temperature, humidity) to ensure that the nanoparticles remain stable during storage and after exposure to the GI environment.
4.4 Formulation Optimization
4.4.1 Coating for GI Protection
- 4.4.1.1 Consider coating the nanoparticles with enteric polymers (e.g., Eudragit) to protect the nanoparticles from stomach acid and promote release in the intestine.
4.4.2 Process Optimization
- 4.4.2.1 Adjust formulation parameters (e.g., polymer concentration, stirring speed) to optimize nanoparticle size, drug loading, and release profile.
4.5 Sterility and Storage
4.5.1 Sterilization
- 4.5.1.1 Sterilize the final nanoparticle formulation using sterile filtration (0.22 µm filter) if required by the application.
4.5.2 Storage Conditions
- 4.5.2.1 Store the nanoparticles in airtight, sterile containers at 4°C or room temperature depending on the formulation’s stability data.
5) Abbreviations, if any
- PLGA: Poly(lactic-co-glycolic acid)
- DLS: Dynamic Light Scattering
- HPLC: High-Performance Liquid Chromatography
- API: Active Pharmaceutical Ingredient
6) Documents, if any
- Nanoparticle Oral Delivery Formulation Logbook
7) References, if any
- Protocols for nanoparticle preparation for oral drug delivery
- FDA Guidance on Nanotechnology in Pharmaceuticals
8) SOP Version
Version 1.0
Annexure
Nanoparticle Oral Delivery Formulation Logbook Template
| Date | Batch Number | Nanoparticle Material | Drug Encapsulated | Particle Size | Drug Loading Efficiency | Operator Initials | QA Initials |
|---|---|---|---|---|---|---|---|
| DD/MM/YYYY | Batch Number | Material Name | Drug Name | Size in nm | Efficiency (%) | Operator Name | QA Name |