Targeted Liposomal Delivery of Docetaxel with Enhanced Cellular Uptake and Retention

Publication ID: 24-11857680_0005_PTD
Published: October 28, 2025
Category:Future Evolutions & Paradigm Shifts

Legal Citation

pr1or.art Inc., “Targeted Liposomal Delivery of Docetaxel with Enhanced Cellular Uptake and Retention,” Published Technical Disclosure No. 24-11857680_0005_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857680_0005_PTD
This technical disclosure describes improvements that would be readily apparent to a Person Having Ordinary Skill In The Art (PHOSITA) when considered in combination with the foundational architecture disclosed in U.S. Patent No. 11,857,680.

Summary of the Inventive Concept

A next-generation liposomal composition for targeted delivery of docetaxel to tumour sites, featuring a novel membrane-permeable peptide for enhanced cellular uptake and retention, improved drug loading and stability, and selective binding to cancer cells.

Background and Problem Solved

The original patent disclosed a liposomal composition with high drug loading, but it had limitations in terms of cellular uptake and retention. The new inventive concept addresses these limitations by introducing a novel membrane-permeable peptide that enhances cellular uptake and retention, thereby improving the efficacy of docetaxel delivery.

Detailed Description of the Inventive Concept

The new inventive concept comprises a liposomal composition with a novel membrane-permeable peptide that facilitates cellular uptake and retention of docetaxel. The peptide is conjugated to the liposome surface, allowing for targeted delivery to tumour sites. The liposomal composition also features a combination of ionic and non-ionic surfactants, a pH-sensitive liposome formulation, and a targeting moiety that selectively binds to cancer cells. The novel amino acid-based buffer in the reconstitution buffer ensures optimal pH conditions for drug release.

Novelty and Inventive Step

The new claims introduce a novel membrane-permeable peptide, a pH-sensitive liposome formulation, and a targeting moiety that selectively binds to cancer cells, which are not obvious from the original patent. These features provide a significant improvement in cellular uptake and retention, making the new inventive concept a paradigm shift in targeted liposomal delivery of docetaxel.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept could include using different types of targeting moieties, such as aptamers or small molecules, or modifying the liposome surface with other functional groups to enhance cellular uptake and retention. Variations of the pH-sensitive liposome formulation could also be explored to optimize drug release kinetics.

Potential Commercial Applications and Market

The new inventive concept has significant commercial potential in the oncology market, particularly in the treatment of solid tumours. The targeted delivery of docetaxel could lead to improved efficacy and reduced toxicity, making it an attractive option for cancer patients. The pharmaceutical industry could benefit from this technology, and potential partnerships with biotech companies could accelerate its development and commercialization.

CPC Classifications

SectionClassGroup
A A61 A61K9/127
A A61 A61K9/0019
A A61 A61K9/1277
A A61 A61K31/337
A A61 A61K47/24
A A61 A61K47/26
A A61 A61K47/28

Field of Art

Pharmaceutical Nanotechnology, specifically liposomal drug delivery systems for oncological applications, involving expertise in pharmaceutical formulation, drug encapsulation, and targeted drug delivery techniques

Person of Ordinary Skill (PHOSITA) Profile

A pharmaceutical scientist or biomedical engineer with advanced degrees (PhD/MS) in pharmaceutical sciences, nanotechnology, or chemical engineering, having expertise in liposomal drug formulation, surface modification techniques, and cancer therapeutic delivery strategies

Obviousness Rationale

A PHOSITA would recognize that the PTD's disclosed variations represent predictable extensions of the source patent's liposomal docetaxel technology, utilizing standard pharmaceutical engineering techniques for enhancing drug delivery. The membrane-permeable peptide, targeting moiety, and pH-sensitive formulation are well-established strategies in liposomal drug delivery that would be obvious to implement as incremental improvements to the existing docetaxel liposome composition. These modifications represent standard design choices within the known repertoire of targeted drug delivery approaches.

Obvious Combinations & Variations

Source Patent Element
Liposomal composition with specific docetaxel concentration (0.8-1% w/w)
PTD Variation
Addition of membrane-permeable peptide for enhanced cellular uptake
Obviousness Reasoning
Conjugating targeting peptides to liposome surfaces is a known technique for improving cellular internalization, representing a predictable optimization of drug delivery systems
Source Patent Element
pH-controlled liposomal formulation (pH about 3)
PTD Variation
pH-sensitive liposome design with novel amino acid-based buffer
Obviousness Reasoning
Modifying pH-responsive characteristics is a routine design choice in liposomal drug delivery, with finite and predictable approaches known in the art
Source Patent Element
Liposomal composition with Soya Phosphatidyl Choline and Sodium Cholesteryl Sulfate
PTD Variation
Combination of ionic and non-ionic surfactants with targeting moieties
Obviousness Reasoning
Surface modification of liposomes using additional surfactants and targeting molecules is a standard technique for improving drug delivery specificity
Source Patent Element
Docetaxel liposomal injection targeting tumour site
PTD Variation
Nanoparticle-conjugated antibody for selective cancer cell binding
Obviousness Reasoning
Implementing targeted delivery mechanisms through antibody conjugation is a well-established approach in nanomedicine with predictable implementation strategies
35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857680 and the disclosed variations, a person having ordinary skill in the art would find the claimed liposomal docetaxel delivery system variations obvious and anticipated, as the technical modifications represent routine optimization and combination of known techniques in targeted drug delivery, without requiring inventive insight beyond the ordinary capabilities of a skilled pharmaceutical formulation scientist.

Original Patent Information

Patent NumberUS 11,857,680
TitleComposition of docetaxel liposomal injection with high drug loading
Assignee(s)SHILPA MEDICARE LIMITED