Published Technical Disclosure Archive

Enhanced Docetaxel Liposomal Composition for Targeted Cancer Therapy

Publication ID: 24-11857680_0006_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Docetaxel Liposomal Composition for Targeted Cancer Therapy,” Published Technical Disclosure No. 24-11857680_0006_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857680_0006_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

An improved docetaxel liposomal composition with enhanced stability, increased residence time in blood, and reduced toxicity, enabling more efficient and targeted cancer treatment.

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, and toxicity. The new inventive concept addresses these limitations by introducing a combination of solvents, excipients, and pH adjusting agents to achieve improved stability, increased residence time, and reduced toxicity.

Detailed Description of the Inventive Concept

The new inventive concept comprises a system for preparing a docetaxel liposomal composition with improved stability, comprising a combination of solvents in a specific ratio to achieve more than 90% drug loading. The composition also includes an excipient that facilitates intravenous administration, and a lyoprotectant to preserve the liposomes during lyophilization. The pH of the composition is adjusted to less than 3.5 to enhance stability. The inventive concept also includes a method for increasing the residence time of docetaxel in blood, reducing toxicity, and targeting tumor sites using the improved liposomal composition.

Novelty and Inventive Step

The new claims introduce a novel combination of solvents, excipients, and pH adjusting agents that improve the stability, residence time, and reduce toxicity of the docetaxel liposomal composition, which is not obvious from the original patent. The inventive concept provides a non-obvious solution to the limitations of the original patent.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept may include varying the ratio of solvents, using different excipients or lyoprotectants, or adjusting the pH range. Variations may also include using different types of lipids or cholesterol, or incorporating additional agents to enhance targeting or efficacy.

Potential Commercial Applications and Market

The enhanced docetaxel liposomal composition has significant commercial potential in the cancer therapy market, particularly in the treatment of solid tumors. The improved stability, increased residence time, and reduced toxicity of the composition make it an attractive option for pharmaceutical companies and researchers seeking to develop more effective and targeted cancer treatments.

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 Formulation and Drug Delivery, specifically liposomal drug compositions for cancer therapeutics, involving expertise in pharmaceutical chemistry, drug encapsulation techniques, and nanomedicine

Person of Ordinary Skill (PHOSITA) Profile

A pharmaceutical scientist with advanced degree (PhD/PharmD) specializing in drug delivery systems, having knowledge of liposomal preparation techniques, solvent interactions, drug loading strategies, and cancer therapeutic formulations

Obviousness Rationale

A person skilled in the art would recognize that the PTD represents predictable variations of the source patent's docetaxel liposomal composition by systematically exploring known pharmaceutical formulation techniques. The disclosed modifications represent standard optimization strategies routinely employed in pharmaceutical development to enhance drug delivery performance. The technical variations demonstrate incremental improvements using well-established pharmaceutical engineering principles that would be apparent to a skilled practitioner.

Obvious Combinations & Variations

Source Patent Element
Docetaxel liposomal composition with specific percentage ranges of components
PTD Variation
Introduction of alternative solvents like methanol and tertiary butanol for drug loading
Obviousness Reasoning
Solvent selection is a routine design choice in pharmaceutical formulation, with predictable outcomes for drug encapsulation efficiency known to those skilled in liposomal preparation techniques
Source Patent Element
pH adjustment to enhance liposomal stability
PTD Variation
Extending pH range to less than 3.5 and introducing alternative pH adjusting agents
Obviousness Reasoning
pH optimization is a standard method for improving pharmaceutical formulation stability, representing a predictable variation within established pharmaceutical engineering practices
Source Patent Element
Sucrose as a component in liposomal composition
PTD Variation
Introducing alternative lyoprotectants like trehalose with similar protective mechanisms
Obviousness Reasoning
Selection of lyoprotectants is a known technique in pharmaceutical science, with multiple interchangeable compounds providing equivalent protective functions for liposomal preparations
Source Patent Element
Phospholipid-based liposomal drug delivery system
PTD Variation
Incorporating additional solubilizers like Tween 80 and Span 80
Obviousness Reasoning
Solubilizer selection represents a standard optimization strategy for improving drug dispersibility and bioavailability, utilizing well-understood pharmaceutical engineering principles
Source Patent Element
Docetaxel liposomal composition targeting tumor sites
PTD Variation
Introducing specific pH adjusting agents to enhance targeting mechanisms
Obviousness Reasoning
Modifying pharmaceutical composition parameters to improve targeting is a predictable approach in nanomedicine drug delivery system design
35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857680 and the comprehensive pharmaceutical formulation variations disclosed herein, a person having ordinary skill in the art would find the claimed liposomal docetaxel compositions obvious and lacking inventive step. The systematic exploration of solvent combinations, pH ranges, and component modifications represents routine pharmaceutical engineering optimization that does not rise to the level of non-obvious innovation.

Original Patent Information

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