Lipid & Liposome Bioconjugation Services

Bio-Synthesis provides lipid conjugation, liposome bioconjugation and LNP formulation for lipid–drug and lipid–oligonucleotide conjugates, PEGylated liposomes and targeted delivery systems across discovery, preclinical and diagnostic applications.

LNP & Liposome Experience Ionizable & PEGylated Lipids Custom & OEM / Kit Support Texas, USA

peptide conjugation Overview

What is lipid and liposome bioconjugation? Lipid and liposome bioconjugation is the process of attaching lipids or liposomal carriers to drugs, nucleic acids, peptides, proteins or imaging agents to improve delivery, stability, targeting and pharmacokinetics in therapeutic and diagnostic applications.

Lipid and liposome bioconjugation enables the coupling of small molecules, oligonucleotides, peptides, proteins, and imaging agents to lipid backbones or liposomal carriers. By tuning lipid composition and surface chemistry, these systems support targeted delivery, controlled release, and improved pharmacokinetics for therapeutics and diagnostics.

Bio-Synthesis supports end-to-end lipid conjugation and liposome bioconjugation — from ionizable and cationic lipids to PEGylated and helper lipids, we engineer carrier architectures, conjugation chemistries, and analytics for discovery, preclinical, and diagnostic applications.

Lipid / Liposome Carrier
Ionizable · Cationic · Helper · PEGylated
Conjugation Chemistry
Amide · Maleimide · Click · Electrostatic
Payload
Drug · Oligonucleotide · Protein · Imaging Agent
Therapeutic Delivery

Lipid and liposome carriers for siRNA/ASO, mRNA, and small-molecule delivery, including ionizable and cationic lipid systems designed for in vivo exposure and uptake.

Targeting & Imaging

PEGylated and ligand-decorated liposomes for receptor targeting, plus lipid–dye conjugates and imaging liposomes for optical, MRI, or nuclear imaging workflows.

Analytics & Scale

Method summaries, CoAs, and optional tech transfer packages to support formulation development, preclinical studies, and diagnostic kit or OEM programs.

Lipid & Liposome Bioconjugation Capabilities
  • Lipid–Drug Conjugates (LDCs) for controlled release, depot, and targeted delivery.
  • Lipid–Oligonucleotide Conjugates (siRNA, ASO, DNA/RNA, aptamers) for direct tissue targeting.
  • Lipid–Peptide & Protein Conjugates for receptor targeting, immune modulation, and vaccines.
  • PEGylated & Ligand-Decorated Liposomes for long-circulating and targeted formulations.
  • Ionizable & Cationic Lipid Systems for nucleic acid delivery and complexation.
  • LNP-Style Architectures integrating ionizable lipids, helper lipids, cholesterol, and PEG-lipids.
  • Imaging & Reporter Liposomes containing fluorophores, radiolabels, or MRI agents.
  • Surface-Functionalized Liposomes (biotin, click handles, targeting ligands).
  • Documentation & OEM Support for kit, diagnostic, or platform integration.

Lipid and liposome bioconjugation can be combined with broader lipid conjugation and bioconjugation services and liposome and LNP carrier delivery systems from Bio-Synthesis.

Lipid Classes Used in Lipid Conjugation & Liposome Bioconjugation at Bio-Synthesis

Structural & Helper Lipids
  • DSPC / DPPC / DOPC / POPC — zwitterionic phospholipids forming the structural bilayer.
  • DOPE — helper lipid that promotes endosomal escape and fusion.
  • Cholesterol — increases membrane rigidity, stability, and in vivo performance.
  • PG / PS lipids (e.g., DOPG, DOPS) — provide negative charge and tune colloidal behavior.
Functional & PEGylated Lipids
  • Ionizable lipids (e.g., DLin-MC3-DMA, DODAP) — pH-dependent charge for nucleic acid delivery.
  • Cationic lipids (e.g., DOTAP, DOTMA) — form electrostatic complexes with DNA/RNA.
  • PEG-lipids (e.g., DSPE-PEG) — provide steric stabilization and surface functionality.
  • Reactive PEG-lipids (maleimide, NHS, azide, DBCO) — enable covalent attachment of ligands.

Therapeutic Focus
  • Use ionizable lipids for siRNA/mRNA delivery; tune pKa for endosomal escape.
  • Favor high Tm helper lipids (e.g., DSPC) for serum stability in LNPs.
  • Select PEG-lipids with appropriate PEG length and linker for circulation time and targeting.
Formulation Behavior
  • Balance neutral, charged, and PEGylated components to minimize aggregation.
  • Match lipid composition to the intended manufacturing process (T-junction mixing, microfluidics, etc.).
  • Include stress testing (freeze–thaw, agitation, dilution) as part of development.

Commonly Used Lipids for Lipid Conjugation & Liposome Bioconjugation We Offer

The table below summarizes representative lipids frequently used by Bio-Synthesis and in the broader field for lipid conjugation and liposome bioconjugation. Lipids are grouped by their primary role in the formulation or conjugation strategy.

Lipid / Reagent Class / Role Reactive Group / Feature Typical Use in Bio-Synthesis
DSPE-PEG(2000)-Maleimide PEGylated reactive lipid Maleimide (thiol-reactive) Conjugation of cysteine-containing peptides, antibodies, or proteins to liposomal surfaces.
DSPE-PEG(2000)-NHS PEGylated reactive lipid NHS ester (amine-reactive) Covalent attachment of amine-containing ligands (peptides, small molecules, proteins).
DSPE-PEG(2000)-Azide PEGylated reactive lipid Azide handle Click-ready liposomes for SPAAC/CuAAC with alkyne/DBCO-modified ligands or oligonucleotides.
DSPE-PEG(2000)-DBCO PEGylated reactive lipid Strained alkyne (DBCO) Copper-free click chemistry with azide-bearing ligands or oligonucleotides.
DSPE-PEG(2000)-Biotin PEGylated affinity lipid Biotin Construction of streptavidin-bridged liposomes and surface capture systems.
Cholesterol Helper / structural lipid Rigid sterol Stabilizes bilayers, improves in vivo stability, used broadly in liposomes and LNPs.
Cholesterol-PEG-Maleimide / -NHS Functionalized cholesterol Maleimide or NHS Anchoring ligands to more rigid cholesterol-rich membranes or nanoparticles.
DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine) Structural helper lipid High Tm phospholipid Provides rigid bilayer core in LNP and liposome formulations for improved stability.
DOPC / POPC Structural phospholipids Fluid phosphatidylcholines Base matrix for more fluid liposomes; often blended with cholesterol and PEG-lipids.
DOPE Helper lipid Fusogenic phospholipid Promotes endosomal escape and membrane fusion in delivery formulations.
DOPS / DOPG Negatively charged lipids Carboxylate / phosphoglycerol headgroups Introduce negative charge, tune zeta potential, and support protein binding interfaces.
DOTAP Cationic lipid Permanent positive charge Electrostatic complexation with DNA/RNA; lipoplex and transfection reagent formulations.
DOTMA Cationic lipid Permanent positive charge Component of classical lipofection mixtures for nucleic acid delivery.
DODAP Ionizable lipid pH-responsive amine Used in early LNP-type systems for siRNA encapsulation and endosomal escape.
DLin-MC3-DMA Ionizable lipid pH-responsive tertiary amine Widely used ionizable lipid for siRNA LNPs; supports high encapsulation and potency.
DOTAP-PEG / Ionizable-PEG conjugates PEGylated cationic/ionizable lipids PEG chain plus charged headgroup Improved colloidal stability and circulation for cationic/ionizable lipid-based carriers.
Custom PEG-lipids with click handles Multifunctional lipids Azide, alkyne, tetrazine, etc. Modular attachment of antibodies, peptides, aptamers, or polymers to preformed liposomes.

Additional specialty and proprietary lipids can be integrated on request, including custom PEG lengths, alternative reactive groups, and lipid–polymer hybrids.

Liposome & LNP Design for Bioconjugation

Formulation Architectures
  • Conventional Liposomes built from PC lipids plus cholesterol for small-molecule drugs.
  • PEGylated Liposomes with DSPE-PEG or related lipids to extend circulation time.
  • Targeted Liposomes bearing antibodies, peptides, aptamers, or small-molecule ligands.
  • LNP-Style Systems with ionizable lipid, helper lipid, cholesterol, PEG-lipid for oligonucleotides and mRNA.
Design Considerations
  • Desired particle size, PDI, and surface charge for the target tissue and route of administration.
  • Ratio of ionizable/cationic lipids to helper and PEGylated components for encapsulation vs tolerability.
  • Ligand density and spacer length when using functional PEG-lipids for targeting.
  • Compatibility with sterile filtration, frozen storage, and manufacturing-scale processes.

  • Lipidated siRNA and ASO constructs formulated into LNPs for systemic administration.
  • PEGylated liposomes carrying small-molecule oncology drugs for improved tolerability.
  • Ligand-decorated liposomes targeting tumor, immune, or hepatic receptors.
  • Imaging liposomes loaded with contrast agents and surface-tagged for cell tracking.
Lipid Nanoparticles Encapsulation Project
  • LNP formulation: ONPATTRO (patisiran)
  • Lipid components: Dlin-MC3-DMA, DSPC, cholesterol, DMG-PEG 2000
  • Lipid ratio: 50 : 10 : 38.5 : 1.5
  • Flow rate ratio (Aqueous : Organic): 3 : 1
  • N/P ratio: 3
DLS profile of LNP-siRNA at 12 ml/min flowrate
DLS profile of LNP-siRNA at 12 ml/min flowrate

LNP-siRNA3: Initial RNA concentration 1.1 mg/ml

DLS profile of LNP-siRNA after 5 day storage at 4C
DLS profile of LNP-siRNA at 12 ml/min flowrate
Testing dilution method
DLS profile of LNP-siRNA at 12 ml/min flowrate

LNP-siRNA7, LNP-siRNA8: Initial RNA concentration 1.1 mg/ml

Dilute the LNP-siRNA using dilution buffer within Sunshine chip

DLS profile of LNP-siRNA at 12 ml/min flowrate
Encapsulation efficiency of several LNP-siRNAs we have tested in lab
DLS profile of LNP-siRNA at 12 ml/min flowrate
Conclustion
  • Flow rate at 12 ml/min is good to generate the LNP-siRNA with desirable size, ~120 nm
  • Final concentration of LNP-siRNA is ~ 0.5 mg/ml when encapsulation siRNA solution at 1.1 mg/ml, with aqueous : organic solvent 3:1 ratio
  • LNP-siRNAs are stable at 4C for >5 days (still counting…)
  • Encapsulation efficiency is very high at different flow rate when using Sunshine

Data demonstrating the use of Sunshine formulation parameters to produce high-encapsulation, uniform LNP–siRNA particles with optimized N:P ratios, low PDI, and strong gene-silencing performance.

You can insert full figures, tables, or captions here when ready.

Conjugation Workflows & Chemistries

Lipid / Liposome Carrier
PEG-lipid · Ionizable lipid · Cholesterol
Conjugation Chemistry
NHS · Maleimide · Click · Electrostatic
Payload
Drug · Oligo · Protein · Peptide
Common Conjugation Strategies
  • Amide Coupling (NHS–Amine) for small molecules, peptides, and proteins.
  • Thiol–Maleimide coupling using cysteine-bearing ligands and maleimide-PEG-lipids.
  • Click Chemistry (Azide–Alkyne, SPAAC) with azide- or DBCO-functional lipids.
  • Electrostatic Complexation of nucleic acids with cationic or ionizable lipids.
Workflow Highlights
  • Route selection based on ligand handles (amine, thiol, azide, alkyne, etc.).
  • Control of ligand-to-lipid ratio and surface density on liposomes.
  • Purification by chromatographic and tangential flow methods as appropriate.
  • QC including particle size, encapsulation efficiency, ligand density, and stability.

Lipids / Formulation
Desired lipid types (ionizable, helper, PEG, cholesterol), ratios if known, and any existing compositions.
Payload
Identity (drug, oligo, peptide, protein, imaging agent), available functional groups, and purity.
Design Goals
Target particle size, release profile, targeting strategy, and project phase (discovery to preclinical).
QC & Documentation
Required analytical assays, acceptance criteria, and documentation needs for internal or OEM use.

Technical Summary — Lipid & Liposome Platform

Workflow
  • Initial design review (lipid composition, payload, route, and risk mapping).
  • Conjugation and formulation route scouting, including PEG-lipid and ligand selection.
  • Process development for encapsulation, mixing, and scale-up.
  • Purification and polishing with TFF and chromatographic methods.
  • QC panel and documentation aligned with your program needs.
Controls & Comparators
  • Unconjugated liposomes and free payload controls.
  • Formulations with varied PEG content, ionizable lipid fraction, or ligand density.
  • Cleavable vs non-cleavable linkers and alternative conjugation sites.
  • Functional benchmarks (potency, uptake, stability, and in vitro/in vivo readouts).
Analytics & Documentation
  • Particle size, PDI, zeta potential, and encapsulation efficiency.
  • Lipid composition, ligand density, and residual solvent analysis where applicable.
  • Stability studies under relevant storage and usage conditions.
  • Certificates of Analysis and optional tech transfer packages.

FAQ

What is lipid conjugation and why is it used in drug delivery?

Lipid conjugation refers to attaching a lipid moiety to a drug, nucleic acid, peptide or protein to improve solubility, stability, membrane interaction and in vivo targeting. In drug delivery, lipid conjugates can be formulated into liposomes or lipid nanoparticles (LNPs) to enhance exposure and reduce off-target toxicity.

Which lipid types can you work with?

We regularly work with ionizable lipids, cationic lipids, PEG-lipids (including reactive PEG-lipids), phospholipids (DSPC, DOPC, DPPC, DOPE, etc.), anionic lipids, cholesterol, and specialty or custom lipids provided by clients.

Can you conjugate ligands directly to lipids or liposomes?

Yes. Using NHS, maleimide, azide/alkyne, or other chemistries, we attach peptides, antibodies, aptamers, small molecules, and polymers to PEG-lipids or to liposomal surfaces as required.

Do you support nucleic acid delivery (siRNA, ASO, mRNA)?

We offer lipidated oligonucleotide conjugates and LNP-style formulations using ionizable and helper lipids, with encapsulation and QC workflows tailored to nucleic acid payloads.

Do you support PEGylated liposome conjugation for oncology or mRNA/siRNA delivery?

Yes. We routinely design PEGylated liposome formulations and LNP-style systems using ionizable and helper lipids, cholesterol and PEG-lipids for oncology drugs and RNA therapeutics, including siRNA, ASO and mRNA payloads, with conjugation strategies matched to your target and route of administration.

What information do you need to scope a lipid or liposome project?

At minimum, we need your payload description, preferred or existing lipid composition, intended route of administration, desired particle size range, and target performance metrics (potency, exposure, or assay readout).

Can you handle custom or proprietary lipids under NDA?

Yes. We routinely work under NDA/MSA and can integrate client-supplied proprietary lipids into the formulation or conjugation design, with all materials and data treated as confidential.

Do you provide material suitable for diagnostic kits or OEM use?

We support projects requiring enhanced documentation, lot control, and stability programs suitable for diagnostic kit or OEM environments, and can align release criteria with your internal standards.

Contact

Speak to a Lipid & Liposome Bioconjugation Scientist

Share your lipid composition, payload, application, and performance goals. We will recommend a formulation and conjugation strategy, QC package, and project scope aligned to your discovery, preclinical, or diagnostic needs.

Request a Quote Feasibility Review OEM / Kit Partner Sample Submission
Phone: +1-972-420-8505
Full Name *
Email *
Company / Institution *
Phone *
Payload type *
Lipid system
Project phase
Message
Attach File (optional)

By submitting, you agree to be contacted regarding your request.

Recommended Reading & Bio-Synthesis Resources

  • Allen, T. M. & Cullis, P. R. — Liposomal drug delivery systems and lipid nanoparticle technologies for nucleic acid therapeutics.
  • Khvorova, A. & Watts, J. K. — Oligonucleotide therapeutics: from chemistry to medicine (for LNP and lipid conjugate strategies).
  • G. T. HermansonBioconjugate Techniques, 3rd Ed. — General reference for lipid and surface bioconjugation chemistries.
  • Bio-Synthesis, Inc. — Application notes, technical bulletins, and white papers on lipid and liposome bioconjugation, available on request or via the Bio-Synthesis website.

Why Choose Bio-Synthesis

Trusted by biotech leaders worldwide for over 40+ years of delivering high quality, fast and scalable synthetic biology solutions.