Enhanced Docetaxel Liposomal Composition for Targeted Tumor Delivery

Publication ID: 24-11857680_0001_PTD

Published: October 28, 2025

Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Docetaxel Liposomal Composition for Targeted Tumor Delivery,” Published Technical Disclosure No. 24-11857680_0001_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857680_0001_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

The present invention relates to an improved docetaxel liposomal composition with enhanced stability, targeted tumor delivery, and increased anti-tumor activity. The inventive concept addresses the limitations of the original patent by incorporating a tumor-specific antibody, optimizing the pH, and combining with a second therapeutic agent.

Background and Problem Solved

The original patent disclosed a docetaxel liposomal composition with high drug loading, but it had limitations in terms of stability, residence time in blood, and tumor targeting. The present invention solves these problems by introducing a tumor-specific antibody conjugated to the liposome surface, optimizing the pH to less than 3.2, and combining the composition with a second therapeutic agent.

Detailed Description of the Inventive Concept

The inventive concept comprises a liposomal composition consisting of docetaxel, phospholipids, cholesterol, and a pH adjusting agent. The composition is prepared by mixing docetaxel with a combination of solvents, followed by lyophilization and reconstitution, resulting in a composition with more than 90% drug loading. The pH of the composition is optimized to less than 3.2, thereby improving the stability of the composition. Additionally, the composition is conjugated with a tumor-specific antibody, which increases the drug's residence time in blood and targets the tumor site. The composition can be administered intravenously and can be combined with a second therapeutic agent to increase the anti-tumor activity.

Novelty and Inventive Step

The novelty of the present invention lies in the combination of a tumor-specific antibody conjugated to the liposome surface, the optimized pH, and the combination with a second therapeutic agent. This inventive step provides a significant improvement over the original patent by enhancing the stability, targeted tumor delivery, and anti-tumor activity of the composition.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept include using different tumor-specific antibodies, varying the pH range, and combining with different therapeutic agents. Additionally, the composition can be administered through different routes, such as orally or topically, and can be used to treat different types of cancer.

Potential Commercial Applications and Market

The present invention has significant commercial potential in the pharmaceutical industry, particularly in the treatment of cancer. The targeted tumor delivery and increased anti-tumor activity of the composition make it an attractive option for cancer treatment. The market for cancer treatment is growing rapidly, and the present invention is well-positioned to capture a significant share of this market.

CPC Classifications

Section	Class	Group
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

Section 103 Obviousness Analysis (PHOSITA)

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Field of Art

Pharmaceutical formulations, specifically liposomal drug delivery systems for antineoplastic agents, with expertise in drug encapsulation, surface modification, and targeted drug delivery techniques

Person of Ordinary Skill (PHOSITA) Profile

A pharmaceutical scientist with advanced degrees in pharmaceutical chemistry or chemical engineering, experienced in liposomal drug formulation, familiar with cancer therapeutic strategies, and skilled in drug loading and modification techniques

Obviousness Rationale

A person having ordinary skill would recognize that the PTD's modifications represent predictable variations of the source patent's core liposomal docetaxel composition. The proposed antibody conjugation, pH optimization, and combination therapy are logical extensions of the existing liposomal delivery technology. These variations represent standard approaches in targeted drug delivery that would be apparent to a skilled practitioner seeking to improve the original formulation's performance.

Obvious Combinations & Variations

Source Patent Element

Liposomal docetaxel composition with specific phospholipid and sucrose ratios

PTD Variation

Adding tumor-specific antibody conjugation to liposome surface

Obviousness Reasoning

Surface modification of liposomes with targeting molecules is a well-established technique in drug delivery, representing a predictable optimization of targeting specificity

Source Patent Element

pH range of approximately 3 in original composition

PTD Variation

Further pH optimization to less than 3.2

Obviousness Reasoning

Fine-tuning pH for improved stability is a routine pharmaceutical formulation strategy with predictable outcomes for drug encapsulation

Source Patent Element

Docetaxel liposomal injection targeting tumor sites

PTD Variation

Combining composition with secondary therapeutic agent

Obviousness Reasoning

Combination therapy is a standard oncological approach, representing an obvious method to enhance treatment efficacy using known pharmaceutical strategies

Source Patent Element

High drug loading technique using solvent combination

PTD Variation

Adding solubilizers like Tween 80 and Span 80

Obviousness Reasoning

Selection of additional solubilization agents is a predictable optimization within established pharmaceutical formulation techniques

Source Patent Element

Liposomal composition with defined component percentages

PTD Variation

Alternative administration routes beyond intravenous

Obviousness Reasoning

Exploring multiple administration routes is a standard pharmaceutical development strategy with predictable design considerations

35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857680, a person having ordinary skill in pharmaceutical formulations would find the variations disclosed in the present technical publication to be obvious extensions of the prior art. The proposed modifications represent predictable refinements in liposomal drug delivery, utilizing known techniques of surface modification, pH optimization, and combination therapy, thereby rendering subsequent claims of novelty invalid under 35 U.S.C. § 103.

Original Patent Information

Patent Number	US 11,857,680
Title	Composition of docetaxel liposomal injection with high drug loading
Assignee(s)	SHILPA MEDICARE LIMITED