APR January/February 2022 - 83

Foam-Forming Compositions
for Delivering an Active to a
Body Cavity;
A.R. Lindal, and D.B.I. Sagna;
Pharmiva AB; Sweden; U.S. Patent#
11,135,166; October 5, 2021.
The patent describes a foam-forming composition for
application to skin, wounds and body cavities. When blown,
it forms a foam and the foam melts at body temperature to
release the content. Foam has low density, which makes the
administration to sensitive areas less painful and it easily
spreads over large surfaces. The formulation contains water,
solid lipid crystals with a melting point between 25°C to
37°C and a non-lipophilic propellent to form the foam. The
foam can be manufactured by two modes. One is during
the manufacturing process by mixing polar gases into the
product and the product is then stored in the form of a foam
at normal pressure. The other way is to introduce a blowing
gas into the formulation and to store the product at elevated
pressure, up to 10 bar, in a pressurized can.
Self-Emulsifying Formulation of
Bisphosphonates and Associated
Dosage Forms;
X. Yuan, Y. Hui, and T. Zhang; Halo Science
LLC, US; U.S. Patent # 11,173,169;
November 16, 2021.
Bisphosphonates are therapeutic agents with strong affinity for bones.
Bisphosphonates or " bisphosphonic acids " are used in the diagnosis
and treatment of disorders and conditions related to bone resorption,
calcium metabolism and phosphate metabolism. Bisphosphonates
inhibit the digestion of bone by encouraging osteoclasts to undergo
apoptosis, or cell death, thereby slowing bone loss. Oral administration
of bisphosphonic acids shows adverse gastrointestinal effect. Also,
they have low oral bioavailability. The present invention relates to drug
delivery of novel self-emulsifying formulations of bisphosphonates or
bisphosphonic acids. The invention also relates to dosage forms or other
controlled release drug delivery systems. The self-emulsifying formulation
and controlled release system will modify the interaction between the
active agent and the digestive tract. The self-emulsifying formulation
helps to lessen GI side-effects, but also improves drug bioavailability.
Transdermal Non-Aqueous
Nanoemulgels for Systemic
Delivery of Aromatase Inhibitor;
A.A.N. Sallam, and H.M. Younes;
Qatar University, Qatar; U.S. Patent #
11,185,504; November 30, 2021.
Some breast cancers require estrogen to continue growing.
Aromatase is the enzyme that synthesizes estrogen and
aromatase inhibitors inhibit the enzyme. The present
invention describes non-aqueous nanoemulgels for
topical or transdermal delivery of potent drugs, particularly
aromatase inhibitors such as letrozole and anastrozole.
Nanoemulgel has an emulsion in the nano scale and a
gel base, both combined as a single formulation. The
nanoemulsion part protects the drug from degradation.
The oily phase comprises glyceryl monooleate (GMO)
and isohexadecane and the emulsifying gelling agent is
SEPINEO P 600. The inventors used propylene glycol and
diethylene glycol ethyl ether as cosolvents, the cosolvents
form nanoglobules of the oily dispersed phase.
Capsule for Drug Delivery Systems of
Targeted Tissue-Specific Delivery Type
Using Carbosilane Dendrimer;
M. Suzuki, K. Hatano, S. Yoshida, Y.
Yamashita; Saitama University and
Quarrymen & Co. Inc., Japan; U.S. Patent #
11,160,877; November 2, 2021.
This patent does not discuss a typical hard-shell capsule. The invention
provides an endocytosis enhancing agent by using carbosilane
dendrimer for the drug delivery system; which is stable in the living
body and enables it to specifically deliver the active ingredient to the
target tissue, and it further enhances the incorporation of a compound
having a variety of molecular weight or biopolymers into the cells. In
the patent, a target sequence presented part (TSPP) is composed of a
fluorescent protein, and a protein or peptide for a target tissue specific
delivery; and wherein said endocytosis enhancing agent comprises a
space for containing an aqueous solvent or organic solvent inside of a
capsule being composed of said aggregatable molecule, and said space
encapsulates a protein having molecular weight of 200,000 daltons or
less or peptide dissolved in said aqueous solvent, or a hydrophobic
molecule dissolved in said organic solvent. The capsule has diameter
from 50 to 500 nm.
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APR January/February 2022

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