SOP for Development of Nanoparticle Formulations for Oral Delivery

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

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