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Nano Phytopharmaceutical Development

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Phytopharmaceuticals have been widely used globally since ancient times and acknowledged by healthcare professionals and patients for their superior therapeutic value and fewer side effects compared to modern medicines. However, phytopharmaceuticals need a scientific and methodical pproach to deliver their components and thereby improve patient compliance and treatment adherence. Dose reduction, improved bioavailability, receptor selective binding, and targeted delivery of phytopharmaceuticals can be likely achieved by molding them into specific nano-formulations. In recent decades, nanotechnology-based phytopharmaceuticals have emerged as potential therapeutic candidates for the treatment of various communicable and non-communicable diseases. Nanotechnology combined with phytopharmaceuticals broadens the therapeutic perspective and overcomes problems associated with plant medicine. The therapeutic application of various nano-phytopharmaceuticals in neurological, cardiovascular, pulmonary, and gastro-intestinal disorders emerged as promising therapeutics for many pathological conditions with good compliance and higher acceptance.

Nanoparticulate delivery of drugs can generally improve drugs’ solubility, bioavailability, stability, pharmacological activity, increase target specificity, promote transport across membrane, prolong circulation times, and reduce systemic and organ toxicity. Pure herbal medicines are often considered less effective compared to pure constituents that are mainly demonstrated to have reduced intestinal absorption when administered orally. This is the reason behind the pharmacological activity/loss associated with pure constituents and such problems can be overcome using new drug delivery systems, such as nanotechnology.

Curcumin APPI

Curcumin

Source : Curcuma longa
✅ Patented Nanoformulations
  • Nanosponges – Improved solubility and entrapment efficiency
  • Phytosomes – Enhanced membrane permeability
❌ Limitations of Conventional Curcumin
  • Poor bioavailability
  • Limited chemical stability
  • Short plasma half-life
  • Low gastrointestinal permeability
Physical Chemical Characterization
Material EE Physical characters WATER Solubility (µg/mL) Stability
(6 months)
PS (nm) ZP PDI
API NA 3 20%
Nanosponges 98% 161 -37 0.46 78
(> 26 fold)
94%
Phytosomes 99% 231 -56 0.61 41
(> 14 fold)
91%
In vitro Potency
Category Assay Inhibition, IC50 (µg/mL)
Curcumin API Nanosponges Phytosomes
Anti Oxidant PFRAP 72 52 28
DPPH 18 54 65
Anti Diabetic α-Amylase 39 10 19
α-Glucosidase 56 21 30
Anti Cancer HCT116 126 46 73
MDA-MB 231 264 21 38

Silybin APPI

Silybin Molecule

Silybin

Source : Silybum marianum
✅ Patented Nanoformulations
  • Nanosponges – Boosted cellular uptake and sustained release
  • Phytosomes – Enhanced liver targeting and permeability
❌ Limitations of Conventional Silybin
  • Poor bioavailability
  • Short half life
  • Limited target specificity
  • Low absorption in the GI tract
  • Inconsistent therapeutic outcomes
Physical Chemical Characterization
Material EE Physical characters WATER Solubility (µg/mL) Stability (6 months)
PS (nm) ZP PDI
API NA NA 6 40%
Nanosponges 98% 268 -18.9 0.542 193
(> 30 fold)
95%
Phytosomes 94% 186 -24.6 0.765 98
(> 15 fold)
82%
In vitro Potency
Category Assay Inhibition, IC50 (µg/mL)
Silybin APPI Nanosponges Phytosomes
Anti Oxidant PFRAP 8 2 3
DPPH 69 19 32
Anti Diabetic α-Amylase 14 2 6
α-Glucosidase 5 0.3 3
Anti Cancer HCT116 237 18 65
MDA-MB 231 65 36 14

Resveratrol APPI

Resveratrol

Resveratrol

Source : Red grapes and Polygonum cuspidatum
✅ Patented Nanoformulations
  • Nanosponges – Enhanced water solubility and prolonged release
  • Phytosomes – Improved membrane permeability and metabolic stability
❌ Limitations of Conventional Resveratrol
  • Poor bioavailability
  • Short half life
  • Limited water solubility
  • Low absorption
  • Low stability
Physical Chemical Characterization
Material EE Physical characters WATER Solubility (µg/mL) Stability
(6 months)
PS (nm) ZP PDI
API NA 50 60%
Nanosponges 98% 330 -28.8 0.515 194
(> 4 fold)
95%
Phytosomes 95% 265 -34.6 0.714 140
(> 3 fold)
90%
In vitro Potency
Category Assay Inhibition, IC50 (µg/mL)
Resveratrol APPI Nanosponges Phytosomes
Anti Oxidant PFRAP 21 2 7
DPPH 84 46 40
Anti Diabetic α-Amylase 32 7 14
α-Glucosidase 77 2 8
Anti Cancer HCT116 81 34 3
MDA-MB 231 260 70 52

Quercetin APPI

Quercetin

Quercetin

Source : Fruits, Vegetables, etc.
✅ Patented Nanoformulations
  • Nanosponges – Improved stability and enhanced solubility
  • Phytosomes – Increased cellular uptake and bioefficacy
❌ Limitations of Conventional Quercetin
  • Poor bioavailability
  • Short half life
  • Metabolic instability
  • Low absorption
Physical Chemical Characterization
Material EE Physical characters WATER Solubility (µg/mL) Stability
(60 days)
PS (nm) ZP PDI
API NA 2 30%
Nanosponges 101% 149 -38 0.44 26
(>13 fold)
93%
Phytosomes 92% 102 -42 0.53 34
(>17 fold)
77%
In vitro Potency
Category Assay Inhibition, IC50 (µg/mL)
Quercetin APPI Nanosponges Phytosomes
Anti Oxidant PFRAP 58 20 36
DPPH 90 42 27
Anti Diabetic α-Amylase 11 2 8
α-Glucosidase 41 23 17
Anti Cancer HCT116 219 66 98
MDA-MB 231 116 82 60

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MLR pharma is an emerging pharmaceutical company devoted to the discovery, development and commercialization of innovative , molecular targeted phytopharmaceuticals for diseases with significant unmet needs.

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